A Phase 1 interventional study of GSK2982772 Modified Release and GSK2982772 Immediate Release in Autoimmune Diseases, sponsored by GlaxoSmithKline. Completed at 1 site in United Kingdom. Open to participants aged 18 Years to 65 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2021-08-13.
Sponsored by GlaxoSmithKline · Phase 1, Interventional, and Treatment
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Among 29 studies in Autoimmune Diseases by GlaxoSmithKline — 1 open to participants now, 2 under way, 1 of them phase 3. Autoimmune Diseases · GlaxoSmithKline.
Among the 29 studies in Autoimmune Diseases by GlaxoSmithKline, this one is the 16th largest by enrollment of the 25 interventional ones that give a count, is one of 3 that started in 2017, is one of 10 in phase 1, and was the 23rd registered.
803 studies on the registry are indexed under Autoimmune Diseases; 272 are open to participants now.
Browse Autoimmune Diseases studies →1 of the 29 studies in Autoimmune Diseases by GlaxoSmithKline is open now, in 12 countries. Recruiting first, the newest first:
GlaxoSmithKline · Sites in United States, Argentina, Australia and 15 more countries
Ages 18+
By country, each count listing its studies:
Of the 195 Autoimmune Diseases studies recruiting now, 90 (46%) set no upper age limit and 79 (41%) stop at 75 or younger; 55 take children under 18; 36 take healthy volunteers.
This study: 18 Years to 65 Years · all sexes · healthy volunteers too.
The full table on the hub →This tab as a report to print or save as PDF → With an account.
29 studies; the count open now beside each. This study's row is marked.
First in 2006; this study’s year is marked. 3 started in 2017.
By drug class, each counting the studies that test any of its medicines:
This study's enrollment of 45 is above the median of 40 across 542 interventional studies indexed under Autoimmune Diseases.
Median enrollment 79 across the 25 interventional studies, 2,231 across the 4 observational. Of the 24 that completed or were terminated, 18 (75%) have results posted.
This tab as a report to print or save as PDF → With an account.
GlaxoSmithKline is the lead sponsor of 3,650 studies on the registry; 117 are open to participants now.
Of its 265 completed or terminated interventional studies of FDA-regulated products, 241 (91%) have results posted.
1 of the studies in Autoimmune Diseases by GlaxoSmithKline that are under way reach primary completion within a year, 0 of them phase 3. Phase 3 first, then by date:
| Study | Primary completion |
|---|---|
| NCT06411249GlaxoSmithKlineA Study Describing the Efficacy and Safety of Belimumab Administered in Adult Participants With Early Systemic Lupus Erythematosus (SLE) | 2027-06-29 |
Add it to your calendar (.ics) → With an account.
Among the 29 studies in Autoimmune Diseases by GlaxoSmithKline, from their registry updates:
Nothing recorded among them since 2026-09-25.
This tab as a report to print or save as PDF → With an account.
GSK2982772 is a first-in-class, highly selective, receptor-interacting protein-1 (RIP1) kinase inhibitor being developed for the treatment of inflammatory bowel disease, plaque psoriasis (PsO), rheumatoid arthritis (RA) and other disease conditions. PK data from the first time in human (FTIH) study for GSK2982772 showed that the half life of GSK2982772 was short (approximately 2 to 3 hours). A once daily (QD) formulation would be more convenient from a subject perspective and could offer the advantage of providing a flatter GSK2982772 concentration time profile. Following completion of Parts A and B, it was determined that the slowest minitab formulation provided a PK profile suitable for QD dosing but this formulation was susceptible to a food effect. This study will evaluate the pharmacokinetics of GSK2982772 following administration of different minitab MR formulations in a capsule relative to an IR reference tablet formulation, the pharmacokinetics of selected MR formulation in capsule following repeat doses for 3 days and to compare the pharmacokinetics of GSK2982772 following administration of MR tablet formulations in the fed and fasted state relative to an IR tablet formulation. The study is divided into three parts: Part A will be a non-randomized 6 periods, sequential, 6-way fixed sequence design in which up to 4 MR minitab formulations in a capsule will be evaluated. Periods 1, 2, and 3 will evaluate a slow MR release duration (nominally 24 hours), a fast MR release duration (nominally 10 hours), and IR tablet respectively. Periods 4, 5 and 6 will have flexible dose regimen and it will depend on the outcomes of Period 1 to 3. Subjects will be admitted to the clinic the previous day before dosing. Each in-patient period will consist of 3 days and 2 nights followed by a minimum washout period of 7 days between doses, for both Part A and C. In Part A and C, 16 healthy subjects will be enrolled such that at least 12 evaluable subjects complete the study. Part B will be an open-label, repeat dose study in which the selected MR minitab formulation in capsule will be evaluated. Each in-patient period will consist of 5 days and 4 nights. There will be a minimum of 7 days washout period between the last morning dose of one period and the first dose of the next period. In Part B, 10 healthy subjects will be enrolled such that at least 6 evaluable subjects complete the study. Part C of the study will be a non-randomised 6 period, sequential, fixed sequence crossover design in which MR tablet formulations will be evaluated. Periods 1 and 2 will evaluate single dose administration of a 240 milligram (mg) MR tablet and the 240 mg IR tablet (reference), respectively. Periods 3, 4, 5 and 6 will be flexible and the dosing regimen will be dependent on the outcome of Periods 1 and 2.
Go through the criteria one by one — yes, no or not sure — and take the list to your doctor or the study team. Kept in this browser only.
Exclusion Criteria:
Underlined terms in the criteria open these too. Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Before you join, the study team explains what taking part involves — its purpose, what happens, the risks and possible benefits — and answers your questions, so you can decide freely. Consent is usually recorded on a form (the informed consent form, ICF) signed by you or, where the law allows, by someone legally authorised to decide for you.
You can keep asking questions during the study, you are told of new information that matters, and you can choose to leave at any time.
Weight in kilograms divided by height in metres squared. Example: 70 kg and 1.75 m gives 70 ÷ (1.75 × 1.75) ≈ 22.9.
What counts as overweight or obesity differs between countries (some use lower cut-offs), so go by the range the study states.
Ways of preventing pregnancy. “Highly effective” methods fail less than 1% of the time a year when used correctly — for example an IUD or an implant.
Criteria usually say which methods count and how long to keep using them after the last dose, sometimes for male participants too. Some studies accept a partner’s vasectomy if it was confirmed successful and that person is the participant’s only sexual partner.
Able to become pregnant: from the first period until menopause, unless permanently unable to through surgery (removal of the womb, or of both ovaries or both fallopian tubes).
Criteria for people of childbearing potential usually ask for a negative pregnancy test and for contraception during the study and for a time after it.
Judged by the study doctor to matter for your health or for the study. It is a doctor’s decision, so ask the study team if you are unsure whether something counts.
Two enzymes measured in a routine blood test of the liver. Higher levels can mean the liver is under strain or damaged. SGPT and SGOT are older names for ALT and AST.
Criteria usually give a limit as a multiple of the upper limit of normal (ULN), often higher when cancer has spread to the liver.
The top of the normal range for a blood test, as set by the laboratory that runs it. Each lab prints its own range next to your result.
“≤ 2.5 × ULN” means the result can be up to two and a half times that top value.
A yellow substance made when red blood cells are broken down, which the liver clears. A high level can mean a problem with the liver or the bile ducts.
Criteria often allow more for people with Gilbert’s syndrome, a harmless inherited condition that raises bilirubin.
On an ECG, the QT interval is the time the heart’s lower chambers take to activate electrically and recover in each beat. QTc is that time adjusted for heart rate (QTcF by Fridericia’s formula, QTcB by Bazett’s). Some medicines lengthen it, and a long QTc can raise the risk of a dangerous heart rhythm.
The study may name a correction formula and a limit in milliseconds, often around 450–480.
A drug or device being studied in a clinical trial.
It may be new, or already approved and being studied for another use, dose or form. Criteria often leave out people who took part in another study of one within a recent period, commonly 30 days or five half-lives.
GFR (glomerular filtration rate) is how much blood the kidneys filter each minute. It is usually estimated from a blood test — eGFR, by formulas such as CKD-EPI or MDRD — and some studies ask for it to be measured directly instead. Usually given in mL/min/1.73 m².
Check the method, the units and the minimum the study states. A value of 90 or above is in the normal-or-high range, but kidney damage can show in other tests too.
Hepatitis B is a virus that infects the liver. These are separate tests: HBsAg positive usually means a current infection (a recent vaccination can briefly cause it too); total anti-HBc (HBcAb) positive means an infection now or in the past; HBV DNA measures how much virus is in the blood.
Some studies accept a past infection if HBV DNA is undetectable, sometimes with antiviral medicine during the study. Check what this study allows.
Hepatitis C is a virus that infects the liver. An HCV antibody test can stay positive after an infection has cleared (and is occasionally positive without one); an HCV RNA test shows whether the virus is there now.
After treatment, hepatitis C counts as cured when HCV RNA is still undetectable 12 weeks or more after the treatment ended. Studies often accept people cured this way.
A weakened immune system. It can come from an illness, such as HIV or some blood cancers, or from medicines that turn the immune system down, for example after an organ transplant or for an autoimmune disease; steroids at higher doses count.
Read whether the line is about a condition or about medicines, and which medicines and doses it means.
The human immunodeficiency virus, which weakens the immune system.
Many studies now accept people whose HIV is controlled on treatment, judged by the viral load and the CD4 count. Check the limits this study sets.
Informed consent
Before you join, the study team explains what taking part involves — its purpose, what happens, the risks and possible benefits — and answers your questions, so you can decide freely. Consent is usually recorded on a form (the informed consent form, ICF) signed by you or, where the law allows, by someone legally authorised to decide for you.
You can keep asking questions during the study, you are told of new information that matters, and you can choose to leave at any time.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
BMI (body mass index)
Weight in kilograms divided by height in metres squared. Example: 70 kg and 1.75 m gives 70 ÷ (1.75 × 1.75) ≈ 22.9.
What counts as overweight or obesity differs between countries (some use lower cut-offs), so go by the range the study states.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Contraception
Ways of preventing pregnancy. “Highly effective” methods fail less than 1% of the time a year when used correctly — for example an IUD or an implant.
Criteria usually say which methods count and how long to keep using them after the last dose, sometimes for male participants too. Some studies accept a partner’s vasectomy if it was confirmed successful and that person is the participant’s only sexual partner.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Childbearing potential
Able to become pregnant: from the first period until menopause, unless permanently unable to through surgery (removal of the womb, or of both ovaries or both fallopian tubes).
Criteria for people of childbearing potential usually ask for a negative pregnancy test and for contraception during the study and for a time after it.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Clinically significant
Judged by the study doctor to matter for your health or for the study. It is a doctor’s decision, so ask the study team if you are unsure whether something counts.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
ALT and AST (liver enzymes)
Two enzymes measured in a routine blood test of the liver. Higher levels can mean the liver is under strain or damaged. SGPT and SGOT are older names for ALT and AST.
Criteria usually give a limit as a multiple of the upper limit of normal (ULN), often higher when cancer has spread to the liver.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
ULN (upper limit of normal)
The top of the normal range for a blood test, as set by the laboratory that runs it. Each lab prints its own range next to your result.
“≤ 2.5 × ULN” means the result can be up to two and a half times that top value.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Bilirubin
A yellow substance made when red blood cells are broken down, which the liver clears. A high level can mean a problem with the liver or the bile ducts.
Criteria often allow more for people with Gilbert’s syndrome, a harmless inherited condition that raises bilirubin.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
QT and QTc
On an ECG, the QT interval is the time the heart’s lower chambers take to activate electrically and recover in each beat. QTc is that time adjusted for heart rate (QTcF by Fridericia’s formula, QTcB by Bazett’s). Some medicines lengthen it, and a long QTc can raise the risk of a dangerous heart rhythm.
The study may name a correction formula and a limit in milliseconds, often around 450–480.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Investigational drug or device
A drug or device being studied in a clinical trial.
It may be new, or already approved and being studied for another use, dose or form. Criteria often leave out people who took part in another study of one within a recent period, commonly 30 days or five half-lives.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
GFR and eGFR (kidney filtering)
GFR (glomerular filtration rate) is how much blood the kidneys filter each minute. It is usually estimated from a blood test — eGFR, by formulas such as CKD-EPI or MDRD — and some studies ask for it to be measured directly instead. Usually given in mL/min/1.73 m².
Check the method, the units and the minimum the study states. A value of 90 or above is in the normal-or-high range, but kidney damage can show in other tests too.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Hepatitis B tests
Hepatitis B is a virus that infects the liver. These are separate tests: HBsAg positive usually means a current infection (a recent vaccination can briefly cause it too); total anti-HBc (HBcAb) positive means an infection now or in the past; HBV DNA measures how much virus is in the blood.
Some studies accept a past infection if HBV DNA is undetectable, sometimes with antiviral medicine during the study. Check what this study allows.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Hepatitis C tests
Hepatitis C is a virus that infects the liver. An HCV antibody test can stay positive after an infection has cleared (and is occasionally positive without one); an HCV RNA test shows whether the virus is there now.
After treatment, hepatitis C counts as cured when HCV RNA is still undetectable 12 weeks or more after the treatment ended. Studies often accept people cured this way.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Immunosuppression
A weakened immune system. It can come from an illness, such as HIV or some blood cancers, or from medicines that turn the immune system down, for example after an organ transplant or for an autoimmune disease; steroids at higher doses count.
Read whether the line is about a condition or about medicines, and which medicines and doses it means.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
HIV
The human immunodeficiency virus, which weakens the immune system.
Many studies now accept people whose HIV is controlled on treatment, judged by the viral load and the CD4 count. Check the limits this study sets.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
Subjects in Part A will receive GSK2982772 MR (Period 1, 2, 4, 5 and 6) and GSK2982772 IR (Period 3)
Drug: GSK2982772 Modified Release · Drug: GSK2982772 Immediate Release
Subjects in Part B will receive GSK2982772 MR
Drug: GSK2982772 Modified Release
Subjects in Part C will receive GSK2982772 MR (Period 1, 3, 4, 5 and 6) and GSK2982772 IR (Period 2)
Drug: GSK2982772 Modified Release · Drug: GSK2982772 Immediate Release
GSK2982772 MR will be available as prototype MR minitablet in capsules with unit dose strength of 60 mg in Part A. In Part B, GSK2982772 MR minitablet in capsules with unit dose strength of 15, 30 or 60 mg will be administered by subjects for Days 1 to 3. In Part C, GSK2982772 MR tablet with unit dose strength of 240, 360 or 480 mg will be administered by subjects. GSK2982772 MR will be administered orally with 240 mL of water.
In part A, GSK2982772 IR tablet will be available with unit dose strength of 30 mg and the total dose administered by subjects will be 120 mg (4 tablets of dose strength 30 mg) orally with 240 mL of water. In part C, GSK2982772 IR tablet will be available with unit dose strength of 30 mg and the total dose administered by subjects will be 240 mg (8 tablets of dose strength 30 mg) orally with 240 mL of water.
Area Under the Curve From Time Zero to Infinity (AUC[0-inf]) of GSK2982772 in IR Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-inf). Participants in the 'Safety Population' for whom a Pharmacokinetic (PK) sample was obtained and analyzed were part of PK Population.
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose
AUC(0-inf) of GSK2982772 in MT Formulation :Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-inf).
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Area Under the Curve From Time Zero to the Last Measurable Concentration (AUC[0-t]) of GSK2982772 in IR Formulation : Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t)
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose
AUC(0-t) of GSK2982772 in MT Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t)
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Area Under the Curve From Time Zero to 24 Hours (AUC[0-24]) of GSK2982772 in IR Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24)
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose
AUC(0-24) of GSK2982772 in MT Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24)
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Area Under the Curve From Time Zero to 12 Hours (AUC[0-12]) of GSK2982772 in IR Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-12)
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 hours post-dose
AUC(0-12) of GSK2982772 in MT Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-12)
Time frame: Pre-dose, 2, 4, 6, 8, 10, and 12 hours post-dose
Maximum Observed Concentration (Cmax) of GSK2982772 in IR Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for Cmax
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose
Cmax of GSK2982772 in MT Formulation: Part A
Blood samples were collected from participants at indicated time points and analyzed for Cmax
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Concentration at 12 Hours Post-dose (C12hour) of GSK2982772 in Part A
Blood samples were collected from participants at indicated time points and analyzed for C12hour.
Time frame: 12 hours post-dose
Concentration at 24 Hours Post-dose (C24hour) of GSK2982772 in Part A
Blood samples were collected from participants at indicated time points and analyzed for C24hour.
Time frame: 24 hours post-dose
Relative Bioavailability (Frelformulation) Based on AUC (0-inf) of GSK2982772 in Part A
Blood samples were collected at indicated time points for analysis of Frelformulation. Frelformulation for AUC (0-inf) was calculated as Geometric mean of AUC (0-inf) of MT (test) / Geometric mean of AUC (0-inf) of IR Formulation (reference) multiplied by 100.
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose (reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose (test)
Frelformulation Based on AUC (0-24) of GSK2982772 in Part A
Blood samples were collected at indicated time points for analysis of Frelformulation. Frelformulation for AUC (0-24) was calculated as Geometric mean of AUC (0-24) of MT (test) / Geometric mean of AUC (0-24) of IR Formulation (reference) multiplied by 100.
Time frame: Pre-dose 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose (reference); Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, and 24 hours post-dose (test)
Frelformulation Based on Cmax of GSK2982772 in Part A
Blood samples were collected at indicated time points for analysis of Frelformulation. Frel was calculated as Geometric mean of Cmax of MT Formulation (test)/ Geometric mean of Cmax of IR Formulation (reference) multiplied by 100.
Time frame: Pre-dose,0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose(reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose(test)
Ratio of Cmax to C12hour of GSK2982772 in IR Formulation: Part A
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hour has been presented.
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 24, 26, 28, 30 and 32 hours post-dose
Ratio of Cmax to C12hour of GSK2982772 in MT Formulation: Part A
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hour has been presented.
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Ratio of Cmax to C24hour of GSK2982772 in IR Formulation: Part A
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hour has been presented.
Time frame: Pre-dose 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose
Ratio of Cmax to C24hour of GSK2982772 in MT Formulation: Part A
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hour has been presented.
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Time to Cmax (Tmax) of GSK2982772 in IR Formulation: Part A
Blood samples were collected at indicated time points for analysis of Tmax.
Time frame: Pre-dose 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, and 24 hours post-dose
Tmax of GSK2982772 in MT Formulation: Part A
Blood samples were collected at indicated time points for analysis of Tmax.
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
AUC(0-inf) of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-inf)
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose
AUC(0-inf) of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-inf).
Time frame: Pre-dose, 2, 3, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
AUC(0-t) of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-t).
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose
AUC(0-t) of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-t).
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
AUC(0-24) of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-24)
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose
AUC(0-24) of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-24)
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours post-dose
AUC (0-12) of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-12)
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, and 12 hours post-dose
AUC (0-12) of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of AUC (0-12)
Time frame: Pre-dose, 2, 4, 6, 8, 10, and 12 hours post-dose
Cmax of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of Cmax
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose
Cmax of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of Cmax
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
C12 of GSK2982772 in Part C: Fasted State
Blood samples was collected at indicated time point for analysis of C12
Time frame: 12 hours post-dose
C24 of GSK2982772 in Part C: Fasted State
Blood samples was collected at indicated time point for analysis of C24
Time frame: 24 hours post-dose
Ratio of Cmax to C12hour of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hours has been presented.
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose
Ratio of Cmax to C12hour of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hours has been presented.
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
Ratio of Cmax to C24hour of GSK2982772 for IR Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hours has been presented.
Time frame: Pre-dose,0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose
Ratio of Cmax to C24hour of GSK2982772 for MM Formulation in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hours has been presented.
Time frame: Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
Frelformulation Based on AUC (0-t) of GSK2982772 in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of Frelformulation. Frel for AUC (0-t) was calculated as Geometric mean of AUC (0-t) of MM formulation (test) / Geometric mean of AUC (0-t) of IR Formulation (reference) multiplied by 100.
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose(reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose(test)
Frelformulation Based on AUC (0-24) of GSK2982772 in Part C: Fasted State
Blood samples were collected at indicated time points for analysis of Frelformulation. Frel for AUC (0-24) was calculated as Geometric mean of AUC (0-24) of MM Fasted formulation (test) / Geometric mean of AUC (0-24) of IR Formulation (reference) multiplied by 100.
Time frame: Pre-dose, 0.33, 0.66, 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 hours post-dose(reference); Pre-dose, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours post-dose(test)
Frelformulation Based on AUC (0-inf) of GSK2982772 After a High Fat Meal in Part A
Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC of GSK2982772 after a high fat meal. Frel for AUC (0-inf) was calculated as Geometric mean of AUC (0-inf) of MT Fed formulation (test) / Geometric mean of AUC (0-inf) of MT Fasted Formulation (reference) multiplied by 100.
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
Frelformulation Based on Cmax of GSK2982772 After a High Fat Meal in Part A
Blood samples were collected at indicated time points for analysis of FrelFE based on AUC of GSK2982772 after a high fat meal. Frel for Cmax was calculated as Geometric mean of Cmax of MT Fed formulation (test) / Geometric mean of Cmax of MT Fasted Formulation (reference) multiplied by 100.
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 26, 28, 30 and 32 hours post-dose
AUC(0-24) of GSK2982772 in Part B
Blood samples were collected at indicated time points for analysis of AUC (0-24)
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 1 and Day 3
Cmax of GSK2982772 in Part B
Blood samples were collected at indicated time points for analysis of Cmax
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 1 and Day 3
Tmax of GSK2982772 in Part B
Blood samples were collected at indicated time points for analysis of Tmax
Time frame: Pre-dose 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24 hours on Day 1 and Day 3
AUC (0-24) of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of AUC (0-24)
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, and 24 hours post-dose
Cmax of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of Cmax
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours
C12 of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of C12
Time frame: 12 hours post-dose
AUC(0-t) of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of AUC (0-t)
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
AUC(0-inf) of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of AUC (0-inf) after meal.
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
AUC(0-12) of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of AUC (0-12) after meal.
Time frame: Pre-dose and at 2, 4, 6, 8, 10, and 12 hours post-dose
Frelformulation Based on AUC (0-t) of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC of GSK2982772 after meal. Frel for Auc (0-t) was calculated as Geometric mean of AUC (0-t) of MM Fed formulation (fed) / Geometric mean of AUC (0-t) of MM Fasted Formulation (fasted) multiplied by 100.
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
Frelformulation Based on Cmax of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of Frelformulation based on Cmax of GSK2982772 after meal. Frel for Cmax was calculated as Geometric mean of Cmax of MM Fed formulation (test) / Geometric mean of Cmax of MM Fasted Formulation (reference) multiplied by 100.
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
Tmax of GSK2982772 After Meal in Part C
Blood samples were collected at indicated time points for analysis of Tmax of GSK2982772 after meal.
Time frame: Pre-dose and at 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 22, 24, 26, 28, 30 and 32 hours post-dose
Number of Participants With Adverse Events (AE) and Serious AEs (SAE) in Part A
An AE is any untoward medical occurrence in a clinical study participants, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. A SAE is defined as any untoward medical occurrence that at any dose may result in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly or birth defect and important medical events may jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed before. All participants who receive at least 1 dose of study treatment and were included in Safety Population. Participants will be analyzed according to the treatment they actually received.
Time frame: Up to Day 43
Number of Participants With AE and SAE in Part B
An AE is any untoward medical occurrence in a clinical study participants, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. A SAE is defined as any untoward medical occurrence that at any dose may result in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly or birth defect and important medical events may jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed before.
Time frame: Up to Day 22
Number of Participants With AE and SAE in Part C
An AE is any untoward medical occurrence in a clinical study participants, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. SAE is defined as any untoward medical occurrence that at any dose may result in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly or birth defect and important medical events may jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed before.
Time frame: Up to Day 43
Number of Participants With Emergent Clinical Chemistry Results by Potential Clinical Importance Criteria: Part A
Blood samples were collected for analysis of clinical chemistry parameters like albumin, creatinine, glucose, potassium, sodium, aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), total bilirubin and calcium. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing Baseline value are assumed to have normal baseline value. Clinical chemistry parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 43
Number of Participants With Emergent Hematology Results by Potential Clinical Importance Criteria: Part A
Blood samples were collected to analyze hematology parameters like platelet count, white blood cell (WBC) count, hemoglobin, hematocrit, total neutrophils, and lymphocytes. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing baseline value are assumed to have normal baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 43
Number of Participants Abnormal Urinalysis Dipstick Results: Part A
Urine samples were collected for analysis of specific gravity, potential of hydrogen ions, glucose, protein, blood and ketones by dipstick method. Microscopic examination were performed if blood or protein values were abnormal.
Time frame: Up to Day 43
Number of Participants With Emergent Clinical Chemistry Results by Potential Clinical Importance Criteria: Part B
Blood samples were collected for analysis of clinical chemistry parameters like albumin, creatinine, glucose, potassium, sodium, AST, ALT, ALP, total bilirubin and calcium. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing baseline value are assumed to have normal baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 22
Number of Participants With Emergent Hematology Results by Potential Clinical Importance Criteria: Part B
Blood samples were collected to analyze hematology parameters like platelet count, WBC count, hemoglobin, hematocrit, total neutrophils, and lymphocytes. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing baseline value are assumed to have normal baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 22
Number of Participants Abnormal Urinalysis Dipstick Results: Part B
Urine samples were collected for analysis of specific gravity, potential of hydrogen ions, glucose, protein, blood and ketones by dipstick method. Microscopic examination were performed if blood or protein values were abnormal.
Time frame: Up to Day 22
Number of Participants With Emergent Clinical Chemistry Results by Potential Clinical Importance Criteria: Part C
Blood samples were collected for analysis of clinical chemistry parameters like albumin, creatinine, glucose, potassium, sodium, AST, ALT, ALP, total bilirubin and calcium. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing Baseline value are assumed to have normal Baseline value. Clinical chemistry parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 43
Number of Participants With Emergent Hematology Results by Potential Clinical Importance Criteria: Part C
Blood samples were collected to analyze hematology parameters like platelet count, WBC count, hemoglobin, hematocrit, total neutrophils, and lymphocytes. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing Baseline value are assumed to have normal Baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 43
Number of Participants Abnormal Urinalysis Dipstick Results: Part C
Urine samples were collected for analysis of specific gravity, potential of hydrogen ions, glucose, protein, blood and ketones by dipstick method. Microscopic examination were performed if blood or protein values were abnormal.
Time frame: Up to Day 43
Number of Participants Abnormal Electrocardiogram (ECG) Findings: Part A
Single 12-lead ECGs was obtained using an ECG machine. PR, QRS, QT and Corrected QT (QTc) intervals were measured in semi-supine or supine position. Number of participants with any visit post-Baseline abnormal clinically significant findings and abnormal not clinically significant findings in ECG results has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 43
Number of Participants Abnormal ECG Findings: Part B
Single 12-lead ECGs was obtained using an ECG machine. PR, QRS, QT and QTc intervals were measured in semi-supine or supine position. Number of participants with any visit post-Baseline abnormal clinically significant findings and abnormal not clinically significant findings in ECG results has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 22
Number of Participants Abnormal ECG Findings: Part C
Single 12-lead ECGs was obtained using an ECG machine. PR, QRS, QT and QTc intervals were measured in semi-supine or supine position. Number of participants with any visit post-Baseline abnormal clinically significant findings and abnormal not clinically significant findings in ECG results has been reported. Data for worst-case post-Baseline has been reported.
Time frame: Up to Day 43
Change From Baseline in Blood Pressure: Part A
Systolic blood pressure (SBP) and diastolic blood pressure (DBP) was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Heart Rate: Part A
Heart rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1 Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Respiration Rate: Part A
Respiration rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Body Temperature: Part A
Body temperature was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Blood Pressure: Part B
SBP and DBP was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1 and Day 3: 2 and 12 hours; Pre-dose on Days 2 and 3; Day 4: 24 hours
Change From Baseline in Heart Rate: Part B
Heart rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1 and Day 3: 2 and 12 hours; Pre-dose on Days 2 and 3; Day 4: 24 hours
Change From Baseline in Respiration Rate: Part B
Respiration rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value
Time frame: Baseline (Day 1, Pre-dose), Day 1 and Day 3: 2 and 12 hours; Pre-dose on Days 2 and 3; Day 4 24 hours
Change From Baseline in Body Temperature: Part B
Body temperature was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1 and Day 3: 2 and 12 hours; Pre-dose on Days 2 and 3; Day 4: 24 hours
Change From Baseline in Blood Pressure: Part C
SBP and DBP was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Heart Rate: Part C
Heart rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Respiration Rate: Part C
Respiration rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
Change From Baseline in Body Temperature: Part C
Body temperature was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
Time frame: Baseline (Day 1, Pre-dose), Day 1: 2 and 12 hours; Day 2: 24hours
This was an open label, 3-part, single and repeat dose study conducted in healthy participants to assess modified release (MR) minitablets (MT) in a capsule and MR monolithic matrix (MM) formulations of GSK2982772 compared to immediate release (IR) tablet formulation of GSK2982772.
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 16 | 0 | 0 |
| Completed | 15 | 0 | 0 |
| Not completed | 1 | 0 | 0 |
| Withdrew: Withdrawal by subject | 1 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 15 | 0 | 0 |
| Completed | 13 | 0 | 0 |
| Not completed | 2 | 0 | 0 |
| Withdrew: Adverse event | 1 | 0 | 0 |
| Withdrew: Withdrawal by subject | 1 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 13 | 0 | 0 |
| Completed | 13 | 0 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 13 | 0 | 0 |
| Completed | 13 | 0 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 16 | 0 | 0 |
| Completed | 16 | 0 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 16 | 0 | 0 |
| Completed | 16 | 0 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 16 | 0 | 0 |
| Completed | 16 | 0 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 10 | 0 |
| Completed | 0 | 10 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 10 | 0 |
| Completed | 0 | 10 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 10 | 0 |
| Completed | 0 | 10 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 10 | 0 |
| Completed | 0 | 8 | 0 |
| Not completed | 0 | 2 | 0 |
| Withdrew: Withdrawal by subject | 0 | 2 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 6 | 0 |
| Completed | 0 | 6 | 0 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 15 |
| Completed | 0 | 0 | 15 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 15 |
| Completed | 0 | 0 | 15 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 15 |
| Completed | 0 | 0 | 15 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 15 |
| Completed | 0 | 0 | 15 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 16 |
| Completed | 0 | 0 | 16 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 16 |
| Completed | 0 | 0 | 16 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 16 |
| Completed | 0 | 0 | 16 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 16 |
| Completed | 0 | 0 | 15 |
| Not completed | 0 | 0 | 1 |
| Withdrew: Withdrawal by subject | 0 | 0 | 1 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 15 |
| Completed | 0 | 0 | 15 |
| Not completed | 0 | 0 | 0 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 15 |
| Completed | 0 | 0 | 14 |
| Not completed | 0 | 0 | 1 |
| Withdrew: Withdrawal by subject | 0 | 0 | 1 |
| Milestone | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF |
|---|---|---|---|
| Started | 0 | 0 | 14 |
| Completed | 0 | 0 | 14 |
| Not completed | 0 | 0 | 0 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-inf). Participants in the 'Safety Population' for whom a Pharmacokinetic (PK) sample was obtained and analyzed were part of PK Population.
| Hours*microgram per milliliter | Part A: IR 120mg Fasted |
|---|---|
| Area Under the Curve From Time Zero to Infinity (AUC[0-inf]) of GSK2982772 in IR Formulation: Part A | 6.305 ± 39.4 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-inf).
| Hours*microgram per milliliter | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| AUC(0-inf) of GSK2982772 in MT Formulation :Part A | 3.852 ± 39.4 | 4.482 ± 47.4 | 5.314 ± 39.7 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t)
| Hours*microgram per milliliter | Part A: IR 120mg Fasted |
|---|---|
| Area Under the Curve From Time Zero to the Last Measurable Concentration (AUC[0-t]) of GSK2982772 in IR Formulation : Part A | 6.258 ± 39.2 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-t)
| Hours*microgram per milliliter | Part A: MT-12hour 120mg Fasted | Part A:MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| AUC(0-t) of GSK2982772 in MT Formulation: Part A | 3.805 ± 42.3 | 4.449 ± 49.4 | 4.720 ± 38.4 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24)
| Hours*microgram per milliliter | Part A: IR 120mg Fasted |
|---|---|
| Area Under the Curve From Time Zero to 24 Hours (AUC[0-24]) of GSK2982772 in IR Formulation: Part A | 6.256 ± 39.2 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-24)
| Hours*microgram per milliliter | Part A:MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| AUC(0-24) of GSK2982772 in MT Formulation: Part A | 3.558 ± 43.6 | 4.255 ± 49.4 | 4.580 ± 39.5 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-12)
| Hours*microgram per milliliter | Part A: IR 120mg Fasted |
|---|---|
| Area Under the Curve From Time Zero to 12 Hours (AUC[0-12]) of GSK2982772 in IR Formulation: Part A | 5.967 ± 38.4 |
Blood samples were collected from participants at indicated time points and analyzed for AUC (0-12)
| Hours*microgram per milliliter | Part A:MT-12hour 120mg Fasted | Part A:MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| AUC(0-12) of GSK2982772 in MT Formulation: Part A | 2.106 ± 45.1 | 3.066 ± 47.7 | 3.573 ± 40.8 |
Blood samples were collected from participants at indicated time points and analyzed for Cmax
| Microgram per milliliter | Part A: IR 120mg Fasted |
|---|---|
| Maximum Observed Concentration (Cmax) of GSK2982772 in IR Formulation: Part A | 1.375 ± 40.1 |
Blood samples were collected from participants at indicated time points and analyzed for Cmax
| Microgram per milliliter | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| Cmax of GSK2982772 in MT Formulation: Part A | 0.277 ± 58.8 | 0.439 ± 54.9 | 0.624 ± 49.4 |
Blood samples were collected from participants at indicated time points and analyzed for C12hour.
| Microgram per milliliter | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) | Part A: IR 120mg Fasted |
|---|---|---|---|---|
| Concentration at 12 Hours Post-dose (C12hour) of GSK2982772 in Part A | 0.220 ± 52.6 | 0.209 ± 56.2 | 0.208 ± 53.1 | 0.045 ± 81.7 |
Blood samples were collected from participants at indicated time points and analyzed for C24hour.
| Microgram per milliliter | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) | Part A: IR 120mg Fasted |
|---|---|---|---|---|
| Concentration at 24 Hours Post-dose (C24hour) of GSK2982772 in Part A | 0.058 ± 73.2 | 0.046 ± 69.5 | 0.030 ± 46.6 | 0.006 ± 108.8 |
Blood samples were collected at indicated time points for analysis of Frelformulation. Frelformulation for AUC (0-inf) was calculated as Geometric mean of AUC (0-inf) of MT (test) / Geometric mean of AUC (0-inf) of IR Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part A:120 mg MT-8hr Fasted and 120 mg IR Fasted | Part A:120 mg MT-12hr Fasted and 120 mg IR Fasted |
|---|---|---|
| Relative Bioavailability (Frelformulation) Based on AUC (0-inf) of GSK2982772 in Part A | 72.77 (67.91 to 77.98) | 60.53 (56.15 to 65.24) |
Blood samples were collected at indicated time points for analysis of Frelformulation. Frelformulation for AUC (0-24) was calculated as Geometric mean of AUC (0-24) of MT (test) / Geometric mean of AUC (0-24) of IR Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part A:120 mg MT-8hr Fasted and 120 mg IR Fasted | Part A:120 mg MT-12hr Fasted and 120 mg IR Fasted |
|---|---|---|
| Frelformulation Based on AUC (0-24) of GSK2982772 in Part A | 68.18 (63.98 to 72.64) | 57.54 (54.01 to 61.30) |
Blood samples were collected at indicated time points for analysis of Frelformulation. Frel was calculated as Geometric mean of Cmax of MT Formulation (test)/ Geometric mean of Cmax of IR Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part A:120 mg MT-8hr Fasted and 120 mg IR Fasted | Part A:120 mg MT-12hr Fasted and 120 mg IR Fasted |
|---|---|---|
| Frelformulation Based on Cmax of GSK2982772 in Part A | 32.13 (27.36 to 37.75) | 20.39 (17.41 to 23.89) |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hour has been presented.
| Ratio | Part A: IR 120mg Fasted |
|---|---|
| Ratio of Cmax to C12hour of GSK2982772 in IR Formulation: Part A | 36.485 ± 20.9265 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hour has been presented.
| Ratio | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| Ratio of Cmax to C12hour of GSK2982772 in MT Formulation: Part A | 1.284 ± 0.2468 | 2.265 ± 0.9119 | 3.240 ± 1.2250 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hour has been presented.
| Ratio | Part A: IR 120mg Fasted |
|---|---|
| Ratio of Cmax to C24hour of GSK2982772 in IR Formulation: Part A | 312.851 ± 221.7640 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hour has been presented.
| Ratio | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| Ratio of Cmax to C24hour of GSK2982772 in MT Formulation: Part A | 6.119 ± 5.1507 | 10.790 ± 4.9019 | 22.915 ± 11.7978 |
Blood samples were collected at indicated time points for analysis of Tmax.
| Hours | Part A: IR 120mg Fasted |
|---|---|
| Time to Cmax (Tmax) of GSK2982772 in IR Formulation: Part A | 2.000 (0.67 to 3.00) |
Blood samples were collected at indicated time points for analysis of Tmax.
| Hours | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|
| Tmax of GSK2982772 in MT Formulation: Part A | 10.000 (2.08 to 18.00) | 4.000 (4.00 to 10.00) | 6.000 (4.00 to 10.00) |
Blood samples were collected at indicated time points for analysis of AUC (0-inf)
| Hours*microgram per milliliter | Part C: IR 240mg Fasted |
|---|---|
| AUC(0-inf) of GSK2982772 for IR Formulation in Part C: Fasted State | 14.797 ± 26.3 |
Blood samples were collected at indicated time points for analysis of AUC (0-inf).
| Hours*microgram per milliliter | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| AUC(0-inf) of GSK2982772 for MM Formulation in Part C: Fasted State | 13.417 ± 23.4 | 22.493 ± 51.3 |
Blood samples were collected at indicated time points for analysis of AUC (0-t).
| Hours*microgram per milliliter | Part C: IR 240mg Fasted |
|---|---|
| AUC(0-t) of GSK2982772 for IR Formulation in Part C: Fasted State | 14.621 ± 25.7 |
Blood samples were collected at indicated time points for analysis of AUC (0-t).
| Hours*microgram per milliliter | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| AUC(0-t) of GSK2982772 for MM Formulation in Part C: Fasted State | 9.676 ± 29.6 | 20.009 ± 29.7 |
Blood samples were collected at indicated time points for analysis of AUC (0-24)
| Hours*microgram per milliliter | Part C: IR 240mg Fasted |
|---|---|
| AUC(0-24) of GSK2982772 for IR Formulation in Part C: Fasted State | 14.619 ± 25.7 |
Blood samples were collected at indicated time points for analysis of AUC (0-24)
| Hours*microgram per milliliter | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| AUC(0-24) of GSK2982772 for MM Formulation in Part C: Fasted State | 8.769 ± 30.9 | 18.177 ± 31.5 |
Blood samples were collected at indicated time points for analysis of AUC (0-12)
| Hours*microgram per milliliter | Part C: IR 240mg Fasted |
|---|---|
| AUC (0-12) of GSK2982772 for IR Formulation in Part C: Fasted State | 13.500 ± 26.3 |
Blood samples were collected at indicated time points for analysis of AUC (0-12)
| Hours*microgram per milliliter | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| AUC (0-12) of GSK2982772 for MM Formulation in Part C: Fasted State | 6.096 ± 32.8 | 12.508 ± 40.1 |
Blood samples were collected at indicated time points for analysis of Cmax
| Microgram per milliliter | Part C: IR 240mg Fasted |
|---|---|
| Cmax of GSK2982772 for IR Formulation in Part C: Fasted State | 2.938 ± 25.2 |
Blood samples were collected at indicated time points for analysis of Cmax
| Microgram per milliliter | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| Cmax of GSK2982772 for MM Formulation in Part C: Fasted State | 0.918 ± 34.2 | 2.010 ± 50.1 |
Blood samples was collected at indicated time point for analysis of C12
| Microgram per milliliter | Part C: IR 240mg Fasted | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|---|
| C12 of GSK2982772 in Part C: Fasted State | 0.197 ± 62.9 | 0.346 ± 41.7 | 0.671 ± 42.3 |
Blood samples was collected at indicated time point for analysis of C24
| Microgram per milliliter | Part C: IR 240mg Fasted | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|---|
| C24 of GSK2982772 in Part C: Fasted State | 0.025 ± 54.9 | 0.162 ± 52.6 | 0.351 ± 52.5 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hours has been presented.
| Ratio | Part C: IR 240mg Fasted |
|---|---|
| Ratio of Cmax to C12hour of GSK2982772 for IR Formulation in Part C: Fasted State | 17.158 ± 7.9158 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C12hour. Mean and standard deviation of ratio of Cmax to C12 hours has been presented.
| Ratio | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| Ratio of Cmax to C12hour of GSK2982772 for MM Formulation in Part C: Fasted State | 2.892 ± 1.2572 | 3.551 ± 2.2615 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hours has been presented.
| Ratio | Part C: IR 240mg Fasted |
|---|---|
| Ratio of Cmax to C24hour of GSK2982772 for IR Formulation in Part C: Fasted State | 138.239 ± 76.3996 |
Blood samples were collected at indicated time points for analysis of ratio of Cmax to C24hour. Mean and standard deviation of ratio of Cmax to C24 hours has been presented.
| Ratio | Part C: MM-12h 240mg Fasted | Part C: MM-12h 480mg Fasted |
|---|---|---|
| Ratio of Cmax to C24hour of GSK2982772 for MM Formulation in Part C: Fasted State | 6.026 ± 2.1936 | 7.991 ± 10.6319 |
Blood samples were collected at indicated time points for analysis of Frelformulation. Frel for AUC (0-t) was calculated as Geometric mean of AUC (0-t) of MM formulation (test) / Geometric mean of AUC (0-t) of IR Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part C:MM-12h 240mg Fasted and IR 240mg Fasted |
|---|---|
| Frelformulation Based on AUC (0-t) of GSK2982772 in Part C: Fasted State | 66.18 (61.91 to 70.74) |
Blood samples were collected at indicated time points for analysis of Frelformulation. Frel for AUC (0-24) was calculated as Geometric mean of AUC (0-24) of MM Fasted formulation (test) / Geometric mean of AUC (0-24) of IR Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part C:MM-12h 240mg Fasted and IR 240mg Fasted |
|---|---|
| Frelformulation Based on AUC (0-24) of GSK2982772 in Part C: Fasted State | 59.98 (55.06 to 65.34) |
Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC of GSK2982772 after a high fat meal. Frel for AUC (0-inf) was calculated as Geometric mean of AUC (0-inf) of MT Fed formulation (test) / Geometric mean of AUC (0-inf) of MT Fasted Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part A:120 mg MT-12hour Fed and 120 mg MT-12hour Fasted |
|---|---|
| Frelformulation Based on AUC (0-inf) of GSK2982772 After a High Fat Meal in Part A | 123.64 (115.98 to 131.80) |
Blood samples were collected at indicated time points for analysis of FrelFE based on AUC of GSK2982772 after a high fat meal. Frel for Cmax was calculated as Geometric mean of Cmax of MT Fed formulation (test) / Geometric mean of Cmax of MT Fasted Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part A:120 mg MT-12hour Fed and 120 mg MT-12hour Fasted |
|---|---|
| Frelformulation Based on Cmax of GSK2982772 After a High Fat Meal in Part A | 225.07 (201.78 to 251.04) |
Blood samples were collected at indicated time points for analysis of AUC (0-24)
| Hours*microgram/milliliter | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Day 1, n=10, 9, 5 | 4.669 ± 26.5 | 8.807 ± 34.3 | 9.662 ± 33.8 |
| Day 3, n=10, 10, 6 | 5.010 ± 32.0 | 9.867 ± 30.4 | 10.948 ± 37.7 |
Blood samples were collected at indicated time points for analysis of Cmax
| Microgram/milliliter | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Day 1 | 0.417 ± 25.5 | 0.707 ± 44.7 | 0.888 ± 14.1 |
| Day 3 | 0.398 ± 32.9 | 0.794 ± 35.7 | 1.080 ± 40.4 |
Blood samples were collected at indicated time points for analysis of Tmax
| Hours | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Day 1 | 4.058 (4.00 to 10.00) | 4.067 (4.00 to 12.00) | 4.000 (4.00 to 10.00) |
| Day 3 | 4.000 (2.00 to 16.0) | 5.025 (4.00 to 20.00) | 4.000 (4.00 to 6.00) |
Blood samples were collected at indicated time points for analysis of AUC (0-24)
| Hours*microgram/milliliter | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| AUC (0-24) of GSK2982772 After Meal in Part C | 17.505 ± 29.5 | 8.734 ± 47.4 | 21.543 ± 39.2 |
Blood samples were collected at indicated time points for analysis of Cmax
| Microgram/milliliter | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| Cmax of GSK2982772 After Meal in Part C | 1.547 ± 40.8 | 1.064 ± 62.6 | 3.151 ± 32.5 |
Blood samples were collected at indicated time points for analysis of C12
| Microgram/milliliter | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| C12 of GSK2982772 After Meal in Part C | 0.706 ± 72.7 | 0.739 ± 37.1 | 0.317 ± 49.5 |
Blood samples were collected at indicated time points for analysis of AUC (0-t)
| Hours*microgram/milliliter | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| AUC(0-t) of GSK2982772 After Meal in Part C | 19.147 ± 28.0 | 9.202 ± 46.4 | 22.712 ± 36.2 |
Blood samples were collected at indicated time points for analysis of AUC (0-inf) after meal.
| Hours*microgram/milliliter | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| AUC(0-inf) of GSK2982772 After Meal in Part C | 18.941 ± 36.5 | 9.995 ± 62.4 | 24.367 ± 49.2 |
Blood samples were collected at indicated time points for analysis of AUC (0-12) after meal.
| Hours*microgram/milliliter | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| AUC(0-12) of GSK2982772 After Meal in Part C | 17.111 ± 45.0 | 10.241 ± 45.9 | 6.771 ± 56.7 |
Blood samples were collected at indicated time points for analysis of Frelformulation based on AUC of GSK2982772 after meal. Frel for Auc (0-t) was calculated as Geometric mean of AUC (0-t) of MM Fed formulation (fed) / Geometric mean of AUC (0-t) of MM Fasted Formulation (fasted) multiplied by 100.
| Percentage bioavailability | Part C:480mg MM-12hour Delayed Fed and 480 mg MM-12hour Fasted | Part C:480mg MM-12hour Fed and 480 mg MM- 12hour Fasted | Part C:240mg MM-12hour Delayed Fed and 240mg MM-12hour Fasted |
|---|---|---|---|
| Frelformulation Based on AUC (0-t) of GSK2982772 After Meal in Part C | 94.69 (87.03 to 103.04) | 113.51 (104.52 to 123.27) | 91.13 (82.23 to 100.98) |
Blood samples were collected at indicated time points for analysis of Frelformulation based on Cmax of GSK2982772 after meal. Frel for Cmax was calculated as Geometric mean of Cmax of MM Fed formulation (test) / Geometric mean of Cmax of MM Fasted Formulation (reference) multiplied by 100.
| Percentage bioavailability | Part C:480mg MM-12hour Delayed Fed and 480 mg MM-12hour Fasted | Part C:480mg MM-12hour Fed and 480 mg MM- 12hour Fasted | Part C:240mg MM-12hour Delayed Fed and 240mg MM-12hour Fasted |
|---|---|---|---|
| Frelformulation Based on Cmax of GSK2982772 After Meal in Part C | 76.56 (64.25 to 91.22) | 156.77 (132.06 to 186.09) | 113.81 (94.00 to 137.78) |
Blood samples were collected at indicated time points for analysis of Tmax of GSK2982772 after meal.
| Hours | Part C MM-12h 480mg Delayed Fed (Standard) | Part C MM-12h 240mg Delayed Fed (High Fat) | Part C MM-12h 480mg Fed (Standard) |
|---|---|---|---|
| Tmax of GSK2982772 After Meal in Part C | 4.000 (2.00 to 20.00) | 4.000 (2.00 to 10.02) | 5.017 (4.00 to 10.00) |
An AE is any untoward medical occurrence in a clinical study participants, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. A SAE is defined as any untoward medical occurrence that at any dose may result in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly or birth defect and important medical events may jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed before. All participants who receive at least 1 dose of study treatment and were included in Safety Population. Participants will be analyzed according to the treatment they actually received.
| Participants | Part A: IR 120mg Fasted | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|---|
| Any AEs | 4 | 5 | 1 | 2 |
| Any SAEs | 0 | 1 | 0 | 0 |
An AE is any untoward medical occurrence in a clinical study participants, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. A SAE is defined as any untoward medical occurrence that at any dose may result in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly or birth defect and important medical events may jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed before.
| Participants | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Any AEs | 1 | 3 | 1 |
| Any SAEs | 0 | 0 | 0 |
An AE is any untoward medical occurrence in a clinical study participants, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. SAE is defined as any untoward medical occurrence that at any dose may result in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly or birth defect and important medical events may jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed before.
| Participants | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Any AEs | 3 | 3 | 3 | 4 | 2 | 1 |
| Any SAEs | 0 | 0 | 0 | 0 | 0 | 0 |
Blood samples were collected for analysis of clinical chemistry parameters like albumin, creatinine, glucose, potassium, sodium, aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), total bilirubin and calcium. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing Baseline value are assumed to have normal baseline value. Clinical chemistry parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) | Part A: IR 120mg Fasted |
|---|---|---|---|---|
| ALT, low | 0 | 0 | 0 | 0 |
| ALT, normal or no change | 16 | 13 | 16 | 16 |
| ALT, high | 0 | 0 | 0 | 0 |
| Albumin, low | 0 | 0 | 0 | 0 |
| Albumin, normal or no change | 16 | 13 | 16 | 16 |
| Albumin, high | 0 | 0 | 0 | 0 |
| ALP, low | 0 | 0 | 0 | 0 |
| ALP, normal or no change | 16 | 13 | 16 | 16 |
| ALP, high | 0 | 0 | 0 | 0 |
| AST, low | 0 | 0 | 0 | 0 |
| AST, normal or no change | 16 | 13 | 16 | 16 |
| AST, high | 0 | 0 | 0 | 0 |
| Calcium, low | 0 | 0 | 0 | 0 |
| Calcium, normal or no change | 16 | 13 | 16 | 16 |
| Calcium, high | 0 | 0 | 0 | 0 |
| Creatinine, low | 0 | 0 | 0 | 0 |
| Creatinine, normal or no change | 16 | 13 | 16 | 16 |
| Creatinine, high | 0 | 0 | 0 | 0 |
| Glucose, low | 0 | 0 | 0 | 0 |
| Glucose, normal or no change | 16 | 13 | 16 | 16 |
| Glucose, high | 0 | 0 | 0 | 0 |
| Potassium, low | 0 | 0 | 0 | 0 |
| Potassium, normal or no change | 15 | 13 | 16 | 15 |
| Potassium, high | 1 | 0 | 0 | 1 |
| Sodium, low | 0 | 0 | 0 | 0 |
| Sodium, normal or no change16 | 16 | 13 | 16 | 16 |
| Sodium, high | 0 | 0 | 0 | 0 |
| Total Bilirubin, low | 0 | 0 | 0 | 0 |
| Total Bilirubin, normal or no change | 16 | 13 | 16 | 16 |
| Total Bilirubin, high | 0 | 0 | 0 | 0 |
Blood samples were collected to analyze hematology parameters like platelet count, white blood cell (WBC) count, hemoglobin, hematocrit, total neutrophils, and lymphocytes. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing baseline value are assumed to have normal baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) | Part A: IR 120mg Fasted |
|---|---|---|---|---|
| Hematocrit, low | 0 | 0 | 0 | 0 |
| Hematocrit, normal or no change | 16 | 13 | 16 | 16 |
| Hematocrit, high | 0 | 0 | 0 | 0 |
| Hemoglobin, low | 0 | 0 | 0 | 0 |
| Hemoglobin, normal or no change | 16 | 13 | 16 | 16 |
| Hemoglobin, high | 0 | 0 | 0 | 0 |
| Lymphocytes, low | 0 | 0 | 0 | 0 |
| Lymphocytes, normal or no change | 16 | 13 | 16 | 16 |
| Lymphocytes, high | 0 | 0 | 0 | 0 |
| Platelet count, low | 0 | 0 | 0 | 0 |
| Platelet count, normal or no change | 16 | 13 | 16 | 16 |
| Platelet count, high | 0 | 0 | 0 | 0 |
| Total Neutrophils, low | 1 | 2 | 0 | 0 |
| Total Neutrophils, normal or no change | 15 | 11 | 16 | 16 |
| Total Neutrophils, high | 0 | 0 | 0 | 0 |
| WBC, low | 1 | 1 | 0 | 0 |
| WBC, normal or no change | 15 | 12 | 16 | 16 |
| WBC, high | 0 | 0 | 0 | 0 |
Urine samples were collected for analysis of specific gravity, potential of hydrogen ions, glucose, protein, blood and ketones by dipstick method. Microscopic examination were performed if blood or protein values were abnormal.
| Participants | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) | Part A: IR 120mg Fasted |
|---|---|---|---|---|
| Number of Participants Abnormal Urinalysis Dipstick Results: Part A | 0 | 0 | 0 | 0 |
Blood samples were collected for analysis of clinical chemistry parameters like albumin, creatinine, glucose, potassium, sodium, AST, ALT, ALP, total bilirubin and calcium. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing baseline value are assumed to have normal baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| ALT, low | 0 | 0 | 0 |
| ALT, normal or no change | 10 | 10 | 6 |
| ALT, high | 0 | 0 | 0 |
| Albumin, low | 0 | 0 | 0 |
| Albumin, normal or no change | 10 | 10 | 6 |
| Albumin, high | 0 | 0 | 0 |
| ALP, low | 0 | 0 | 0 |
| ALP, normal or no change | 10 | 10 | 6 |
| ALP, high | 0 | 0 | 0 |
| AST, low | 0 | 0 | 0 |
| AST, normal or no change | 10 | 10 | 6 |
| AST, high | 0 | 0 | 0 |
| Calcium, low | 0 | 0 | 0 |
| Calcium, normal or no change | 10 | 10 | 6 |
| Calcium, high | 0 | 0 | 0 |
| Creatinine, low | 0 | 0 | 0 |
| Creatinine, normal or no change | 10 | 10 | 6 |
| Creatinine, high | 0 | 0 | 0 |
| Glucose, low | 0 | 0 | 0 |
| Glucose, normal or no change | 10 | 10 | 6 |
| Glucose, high | 0 | 0 | 0 |
| Potassium, low | 0 | 0 | 0 |
| Potassium, normal or no change | 10 | 10 | 6 |
| Potassium, high | 0 | 0 | 0 |
| Sodium, low | 0 | 0 | 0 |
| Sodium, normal or no change | 10 | 10 | 6 |
| Sodium, high | 0 | 0 | 0 |
| Total Bilirubin, low | 0 | 0 | 0 |
| Total Bilirubin, normal or no change | 10 | 10 | 6 |
| Total Bilirubin, high | 0 | 0 | 0 |
Blood samples were collected to analyze hematology parameters like platelet count, WBC count, hemoglobin, hematocrit, total neutrophils, and lymphocytes. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the subject has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing baseline value are assumed to have normal baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Hematocrit, low | 0 | 0 | 0 |
| Hematocrit, normal or no change | 10 | 10 | 6 |
| Hematocrit, high | 0 | 0 | 0 |
| Hemoglobin, low | 0 | 0 | 0 |
| Hemoglobin, normal or no change | 10 | 10 | 6 |
| Hemoglobin, high | 0 | 0 | 0 |
| Lymphocytes, low | 0 | 0 | 0 |
| Lymphocytes, normal or no change | 10 | 10 | 6 |
| Lymphocytes, high | 0 | 0 | 0 |
| Platelet count, low | 0 | 0 | 0 |
| Platelet count, normal or no change | 10 | 10 | 6 |
| Platelet count, high | 0 | 0 | 0 |
| Total Neutrophils, low | 0 | 0 | 0 |
| Total Neutrophils, normal or no change | 10 | 10 | 6 |
| Total Neutrophils, high | 0 | 0 | 0 |
| WBC, low | 0 | 0 | 0 |
| WBC, normal or no change | 10 | 10 | 6 |
| WBC, high | 0 | 0 | 0 |
Urine samples were collected for analysis of specific gravity, potential of hydrogen ions, glucose, protein, blood and ketones by dipstick method. Microscopic examination were performed if blood or protein values were abnormal.
| Participants | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Number of Participants Abnormal Urinalysis Dipstick Results: Part B | 0 | 0 | 0 |
Blood samples were collected for analysis of clinical chemistry parameters like albumin, creatinine, glucose, potassium, sodium, AST, ALT, ALP, total bilirubin and calcium. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing Baseline value are assumed to have normal Baseline value. Clinical chemistry parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| ALT, low | 0 | 0 | 0 | 0 | 0 | 0 |
| ALT, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| ALT, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Albumin, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Albumin, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Albumin, high | 0 | 0 | 0 | 0 | 0 | 0 |
| ALP, low | 0 | 0 | 0 | 0 | 0 | 0 |
| ALP, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| ALP, high | 0 | 0 | 0 | 0 | 0 | 0 |
| AST, low | 0 | 0 | 0 | 0 | 0 | 0 |
| AST, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| AST, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Calcium, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Calcium, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Calcium, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Creatinine, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Creatinine, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Creatinine, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Glucose, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Glucose, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Glucose, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Potassium, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Potassium, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Potassium, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Sodium, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Sodium, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Sodium, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Total Bilirubin, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Total Bilirubin, normal or no change | 15 | 15 | 15 | 16 | 14 | 14 |
| Total Bilirubin, high | 0 | 0 | 1 | 0 | 1 | 14 |
Blood samples were collected to analyze hematology parameters like platelet count, WBC count, hemoglobin, hematocrit, total neutrophils, and lymphocytes. Participants are counted in the worst case category that their value changes to (Low, Normal or High), unless there is no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the "To Normal or No Change" category. Participants are counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. Participants with missing Baseline value are assumed to have normal Baseline value. Hematology parameters with potential clinical importance data has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Hematocrit, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Hematocrit, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Hematocrit, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Hemoglobin, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Hemoglobin, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Hemoglobin, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Lymphocytes, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Lymphocytes, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Lymphocytes, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Platelet count, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Platelet count, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Platelet count, high | 0 | 0 | 0 | 0 | 0 | 0 |
| Total Neutrophils, low | 0 | 0 | 0 | 0 | 0 | 0 |
| Total Neutrophils, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| Total Neutrophils, high | 0 | 0 | 0 | 0 | 0 | 0 |
| WBC, low | 0 | 0 | 0 | 0 | 0 | 0 |
| WBC, normal or no change | 15 | 15 | 16 | 16 | 15 | 14 |
| WBC, high | 0 | 0 | 0 | 0 | 0 | 0 |
Urine samples were collected for analysis of specific gravity, potential of hydrogen ions, glucose, protein, blood and ketones by dipstick method. Microscopic examination were performed if blood or protein values were abnormal.
| Participants | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Number of Participants Abnormal Urinalysis Dipstick Results: Part C | 0 | 0 | 0 | 0 | 0 | 0 |
Single 12-lead ECGs was obtained using an ECG machine. PR, QRS, QT and Corrected QT (QTc) intervals were measured in semi-supine or supine position. Number of participants with any visit post-Baseline abnormal clinically significant findings and abnormal not clinically significant findings in ECG results has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) | Part A: IR 120mg Fasted |
|---|---|---|---|---|
| Abnormal, not clinically significant | 6 | 8 | 9 | 9 |
| Abnormal, clinically significant | 1 | 0 | 0 | 0 |
Single 12-lead ECGs was obtained using an ECG machine. PR, QRS, QT and QTc intervals were measured in semi-supine or supine position. Number of participants with any visit post-Baseline abnormal clinically significant findings and abnormal not clinically significant findings in ECG results has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Abnormal, not clinically significant | 4 | 4 | 2 |
| Abnormal, clinically significant | 0 | 0 | 0 |
Single 12-lead ECGs was obtained using an ECG machine. PR, QRS, QT and QTc intervals were measured in semi-supine or supine position. Number of participants with any visit post-Baseline abnormal clinically significant findings and abnormal not clinically significant findings in ECG results has been reported. Data for worst-case post-Baseline has been reported.
| Participants | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Abnormal, not clinically significant | 1 | 4 | 7 | 5 | 6 | 3 |
| Abnormal, clinically significant | 0 | 0 | 0 | 0 | 0 | 0 |
Systolic blood pressure (SBP) and diastolic blood pressure (DBP) was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Millimeters of mercury | Part A: IR 120mg Fasted | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|---|
| SBP, Day 1, 2 hours, n=16,16, 13,16 | -1.4 ± 13.46 | 4.3 ± 10.70 | -0.2 ± 16.53 | -6.2 ± 11.20 |
| SBP,Day 1, 12 hours, n=15,16, 13,16 | -1.6 ± 14.05 | -2.5 ± 14.27 | -6.2 ± 12.34 | -2.9 ± 18.70 |
| SBP,Day 2, 24 hours, n=16,16, 13,16 | 7.4 ± 13.86 | -2.7 ± 9.76 | -6.2 ± 11.22 | -3.9 ± 14.11 |
| DBP, Day 1, 2 hours, n=16,16, 13,16 | 0.3 ± 7.33 | 3.0 ± 8.12 | -1.8 ± 7.81 | -4.4 ± 8.94 |
| DBP,Day 1, 12 hours, n=16,16, 13,16 | -3.9 ± 10.01 | -3.6 ± 9.87 | -3.0 ± 9.27 | -3.9 ± 9.02 |
| DBP,Day 2, 24 hours, n=16,16, 13,16 | 2.1 ± 8.51 | 0.7 ± 7.60 | -1.7 ± 7.79 | -1.1 ± 8.82 |
Heart rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Beats per minute | Part A: IR 120mg Fasted | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|---|
| Day 1, 2 hours | -4.4 ± 5.11 | -0.3 ± 4.88 | -2.5 ± 7.62 | 3.9 ± 7.48 |
| Day 1, 12 hours | 4.8 ± 6.06 | 5.2 ± 3.94 | 5.8 ± 5.57 | 7.5 ± 9.93 |
| Day 2, 24 hours | 1.5 ± 9.41 | -2.1 ± 6.31 | 0.6 ± 7.14 | 0.9 ± 7.62 |
Respiration rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value
| Breaths per minute | Part A: IR 120mg Fasted | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|---|
| Day 1, 2 hours | -0.4 ± 1.67 | 0.8 ± 1.65 | 0.0 ± 1.00 | -1.5 ± 2.50 |
| Day 1, 12 hours | -0.6 ± 1.71 | -0.1 ± 1.82 | -0.2 ± 1.21 | -2.4 ± 2.63 |
| Day 2, 24 hours | 1.3 ± 2.15 | -0.1 ± 1.54 | -1.5 ± 1.51 | -1.4 ± 2.13 |
Body temperature was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Degree Celsius | Part A: IR 120mg Fasted | Part A: MT-12hour 120mg Fasted | Part A: MT-8hour 120mg Fasted | Part A: MT-12hour 120mg Fed (High Fat) |
|---|---|---|---|---|
| Day 1, 2 hours | 0.02 ± 0.152 | 0.18 ± 0.180 | 0.05 ± 0.145 | 0.14 ± 0.126 |
| Day 1, 12 hours | 0.07 ± 0.139 | -0.04 ± 0.145 | 0.13 ± 0.118 | 0.11 ± 0.173 |
| Day 2, 24 hours | 0.04 ± 0.182 | 0.07 ± 0.095 | 0.12 ± 0.114 | 0.12 ± 0.161 |
SBP and DBP was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Millimeters of mercury | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| SBP, Day 1, 2 hours | -0.5 ± 7.40 | 5.4 ± 7.37 | 1.2 ± 7.08 |
| SBP,Day 1, 12 hours | 2.7 ± 7.75 | 1.5 ± 8.86 | 1.0 ± 10.73 |
| SBP,Day 2, Pre-dose | -0.1 ± 5.26 | 3.5 ± 7.76 | 1.8 ± 6.62 |
| SBP,Day 3, Pre-dose | -1.0 ± 9.35 | 1.1 ± 5.09 | -0.7 ± 14.09 |
| SBP,Day 3, 2 hours | 2.0 ± 8.37 | 5.5 ± 9.51 | -3.3 ± 9.14 |
| SBP,Day 3, 12 hours | 2.4 ± 11.55 | 7.4 ± 14.17 | 3.8 ± 8.21 |
| SBP,Day 4, 24 hours | 2.9 ± 9.22 | 6.1 ± 5.04 | 6.0 ± 11.24 |
| DBP, Day 1, 2 hours | 2.4 ± 7.31 | 2.1 ± 7.16 | -4.0 ± 4.20 |
| DBP,Day 1, 12 hours | -1.7 ± 5.50 | -2.2 ± 4.59 | -5.7 ± 4.03 |
| DBP,Day 2, Pre-dose | -1.5 ± 4.55 | 2.0 ± 7.47 | -2.7 ± 6.56 |
| DBP,Day 3, Pre-dose | 2.6 ± 8.57 | 1.3 ± 6.65 | 1.3 ± 4.50 |
| DBP,Day 3, 2 hours | 3.1 ± 7.00 | 4.0 ± 5.31 | -5.8 ± 3.87 |
| DBP,Day 3, 12 hours | -1.4 ± 7.78 | -1.4 ± 5.72 | -2.5 ± 2.81 |
| DBP,Day 4, 24 hours | 3.0 ± 5.56 | 4.6 ± 4.77 | 1.3 ± 6.65 |
Heart rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Beats per minute | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Day 1, 2 hours | 0.0 ± 5.50 | -2.4 ± 5.38 | 7.3 ± 6.89 |
| Day 1, 12 hours | 10.0 ± 4.00 | 8.8 ± 5.22 | 10.5 ± 3.78 |
| Day 2, Pre-dose | -0.1 ± 4.68 | -0.8 ± 6.37 | -1.8 ± 2.71 |
| Day 3, Pre-dose | 2.3 ± 4.74 | -0.1 ± 5.88 | 1.5 ± 5.43 |
| Day 3, 2 hours | 1.2 ± 5.37 | -0.3 ± 5.36 | 4.0 ± 2.28 |
| Day 3, 12 hours | 8.6 ± 4.58 | 10.6 ± 7.26 | 7.7 ± 5.28 |
| Day 4, 24 hours | 4.7 ± 8.64 | 6.7 ± 10.01 | 0.3 ± 2.58 |
Respiration rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value
| Breaths per minute | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Day 1, 2 hours | 0.5 ± 2.27 | -2.0 ± 2.00 | -1.2 ± 3.54 |
| Day 1, 12 hours | -0.1 ± 1.37 | -2.5 ± 2.17 | -1.5 ± 2.35 |
| Day 2, Pre-dose | -0.3 ± 1.49 | -0.5 ± 2.07 | -0.5 ± 2.74 |
| Day 3, Pre-dose | -0.7 ± 2.67 | -0.5 ± 1.43 | 1.5 ± 2.26 |
| Day 3, 2 hours | -1.3 ± 2.36 | -1.0 ± 2.21 | -0.7 ± 2.16 |
| Day 3, 12 hours | 0.3 ± 3.02 | -1.3 ± 2.16 | -0.8 ± 1.33 |
| Day 4, 24 hours | -0.8 ± 1.87 | -1.0 ± 1.89 | -0.3 ± 2.42 |
Body temperature was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Degree Celsius | Part B: MT-12 120mg Fasted | Part B :MT-12 240mg Fasted | Part B :MT-12hour 300mg Fed (Standard) |
|---|---|---|---|
| Day 1, 2 hours | 0.03 ± 0.298 | -0.01 ± 0.233 | 0.00 ± 0.110 |
| Day 1, 12 hours | 0.06 ± 0.181 | 0.08 ± 0.274 | 0.07 ± 0.082 |
| Day 2, Pre-dose | 0.04 ± 0.184 | -0.04 ± 0.158 | 0.12 ± 0.133 |
| Day 3, Pre-dose | 0.04 ± 0.135 | 0.07 ± 0.271 | 0.23 ± 0.151 |
| Day 3, 2 hours | -0.03 ± 0.149 | 0.01 ± 0.260 | -0.08 ± 0.147 |
| Day 3, 12 hours | 0.01 ± 0.191 | 0.05 ± 0.242 | 0.05 ± 0.138 |
| Day 4, 24 hours | 0.04 ± 0.171 | 0.11 ± 0.247 | 0.00 ± 0.089 |
SBP and DBP was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Millimeters of mercury | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| SBP, Day 1, 2 hours | -3.3 ± 7.93 | -0.6 ± 7.50 | -0.6 ± 6.16 | -4.9 ± 9.18 | 1.1 ± 16.02 | -0.2 ± 11.44 |
| SBP,Day1, 12 hours | -3.1 ± 10.04 | -2.6 ± 8.34 | 1.4 ± 12.06 | 0.1 ± 10.81 | -7.3 ± 14.92 | 0.9 ± 16.03 |
| SBP,Day2, 24 hours | 4.9 ± 8.02 | -1.4 ± 6.71 | -1.6 ± 8.39 | -3.1 ± 8.50 | 2.6 ± 10.84 | -7.5 ± 10.58 |
| DBP, Day 1, 2 hours | -0.1 ± 7.41 | -0.7 ± 6.43 | 2.0 ± 6.92 | -4.3 ± 6.94 | -0.6 ± 7.88 | -1.9 ± 5.50 |
| DBP,Day1, 12 hours | -2.1 ± 7.23 | -1.1 ± 6.36 | -3.1 ± 6.53 | -0.6 ± 8.02 | -3.7 ± 9.61 | 0.0 ± 8.38 |
| DBP,Day2, 24 hours | 0.4 ± 7.21 | 1.0 ± 4.88 | -0.5 ± 6.64 | 2.8 ± 6.37 | 0.7 ± 7.49 | 2.4 ± 6.21 |
Heart rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Beats per minute | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Day 1, 2 hours | 2.1 ± 6.94 | -5.3 ± 6.19 | 0.0 ± 6.86 | 7.3 ± 6.56 | 8.2 ± 5.72 | 8.2 ± 7.32 |
| Day 1, 12 hours | 6.8 ± 6.20 | 6.5 ± 9.73 | 11.2 ± 9.65 | 10.3 ± 6.94 | 9.3 ± 8.28 | 8.6 ± 6.99 |
| Day 2, 24 hours | 1.8 ± 5.44 | 0.1 ± 6.41 | -0.4 ± 3.77 | 0.4 ± 5.80 | -0.9 ± 6.19 | 1.6 ± 7.74 |
Respiration rate was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Breaths per minute | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Day 1, 2 hours | 1.7 ± 3.37 | 0.6 ± 2.03 | 0.9 ± 2.90 | -1.1 ± 2.95 | 1.8 ± 1.74 | 0.1 ± 2.76 |
| Day 1, 12 hours | 1.1 ± 2.59 | 1.0 ± 2.85 | 0.6 ± 2.66 | -1.1 ± 2.90 | -0.3 ± 2.61 | 0.5 ± 1.51 |
| Day 2, 24 hours | 1.6 ± 3.25 | 0.4 ± 3.07 | 0.6 ± 4.00 | -2.2 ± 2.66 | 1.8 ± 2.31 | 0.4 ± 3.34 |
Body temperature was measured in semi-supine position. Baseline is defined as the latest pre-dose assessment before entering study. Change from Baseline was defined as post-dose visit value minus Baseline value.
| Degree Celsius | Part C: IR 240mg Fasted | Part C:MM-12h 240mg Fasted | Part C:MM-12h 480mg Fasted | Part C:MM-12h 480mg Fed(Standard) | Part C:MM-12h 480mg Delayed Fed(Standard) | Part C: MM-12h 240mg Delayed Fed(High Fat) |
|---|---|---|---|---|---|---|
| Day 1, 2 hours | -0.10 ± 0.245 | -0.05 ± 0.192 | -0.07 ± 0.215 | 0.23 ± 0.275 | 0.01 ± 0.228 | 0.10 ± 0.301 |
| Day 1, 12 hours | 0.02 ± 0.197 | -0.11 ± 0.229 | -0.05 ± 0.271 | 0.12 ± 0.307 | -0.14 ± 0.241 | -0.10 ± 0.266 |
| Day 2, 24 hours | -0.04 ± 0.256 | 0.15 ± 0.261 | -0.00 ± 0.239 | 0.10 ± 0.278 | -0.09 ± 0.269 | -0.01 ± 0.241 |
Collected over Non-serious AEs and SAEs were collected up to Day 43 for Part A and Part C and up to Day 22 for Part B. Non-serious events are listed at a 0% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Part A:IR 120mg Fasted | 0/16 (0%) | 0/16 (0%) | 4/16 (25%) |
| Part A:MT-12hour 120mg Fasted | 1/16 (6.3%) | 1/16 (6.3%) | 5/16 (31.3%) |
| Part A:MT-8hour 120mg Fasted | 0/13 (0%) | 0/13 (0%) | 1/13 (7.7%) |
| Part A:MT-12hour 120mg Fed (High Fat) | 0/16 (0%) | 0/16 (0%) | 2/16 (12.5%) |
| Part B:MT-12hour 120mg Fasted | 0/10 (0%) | 0/10 (0%) | 1/10 (10%) |
| Part B:MT-12hour 240mg Fasted | 0/10 (0%) | 0/10 (0%) | 3/10 (30%) |
| Part B:MT-12hour 300mg Fed (Standard) | 0/6 (0%) | 0/6 (0%) | 1/6 (16.7%) |
| Part C:IR 240mg Fasted | 0/15 (0%) | 0/15 (0%) | 3/15 (20%) |
| Part C:MM-12hour 240mg Fasted | 0/15 (0%) | 0/15 (0%) | 3/15 (20%) |
| Part C:MM-12hour 480mg Fasted | 0/16 (0%) | 0/16 (0%) | 3/16 (18.8%) |
| Part C:MM-12hour 480mg Fed (Standard) | 0/16 (0%) | 0/16 (0%) | 4/16 (25%) |
| Part C:MM-12hour 480mg Delayed Fed (Standard) | 0/15 (0%) | 0/15 (0%) | 2/15 (13.3%) |
| Part C:MM-12hour 240mg Delayed Fed (High Fat) | 0/14 (0%) | 0/14 (0%) | 1/14 (7.1%) |
| Event | Part A:IR 120mg Fasted | Part A:MT-12hour 120mg Fasted | Part A:MT-8hour 120mg Fasted | Part A:MT-12hour 120mg Fed (High Fat) | Part B:MT-12hour 120mg Fasted | Part B:MT-12hour 240mg Fasted | Part B:MT-12hour 300mg Fed (Standard) | Part C:IR 240mg Fasted | Part C:MM-12hour 240mg Fasted | Part C:MM-12hour 480mg Fasted | Part C:MM-12hour 480mg Fed (Standard) | Part C:MM-12hour 480mg Delayed Fed (Standard) | Part C:MM-12hour 240mg Delayed Fed (High Fat) |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| AsphyxiaRespiratory, thoracic and mediastinal disorders | 0/16 | 1/16 | 0/13 | 0/16 | 0/10 | 0/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| Event | Part A:IR 120mg Fasted | Part A:MT-12hour 120mg Fasted | Part A:MT-8hour 120mg Fasted | Part A:MT-12hour 120mg Fed (High Fat) | Part B:MT-12hour 120mg Fasted | Part B:MT-12hour 240mg Fasted | Part B:MT-12hour 300mg Fed (Standard) | Part C:IR 240mg Fasted | Part C:MM-12hour 240mg Fasted | Part C:MM-12hour 480mg Fasted | Part C:MM-12hour 480mg Fed (Standard) | Part C:MM-12hour 480mg Delayed Fed (Standard) | Part C:MM-12hour 240mg Delayed Fed (High Fat) |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Injury associated with deviceGeneral disorders | 0/16 | 0/16 | 0/13 | 0/16 | 0/10 | 1/10 | 1/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| HeadacheNervous system disorders | 1/16 | 0/16 | 0/13 | 0/16 | 1/10 | 0/10 | 0/6 | 2/15 | 1/15 | 2/16 | 2/16 | 1/15 | 1/14 |
| NasopharyngitisInfections and infestations | 2/16 | 1/16 | 0/13 | 0/16 | 0/10 | 0/10 | 0/6 | 0/15 | 1/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| Back painMusculoskeletal and connective tissue disorders | 0/16 | 2/16 | 0/13 | 1/16 | 0/10 | 0/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| Catheter site bruiseGeneral disorders | 0/16 | 2/16 | 0/13 | 0/16 | 0/10 | 0/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 1/15 | 0/14 |
| Vessel puncture site bruiseGeneral disorders | 0/16 | 0/16 | 0/13 | 0/16 | 1/10 | 0/10 | 0/6 | 0/15 | 0/15 | 1/16 | 0/16 | 1/15 | 0/14 |
| Catheter site painGeneral disorders | 0/16 | 0/16 | 0/13 | 0/16 | 1/10 | 0/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| Catheter site swellingGeneral disorders | 0/16 | 0/16 | 0/13 | 0/16 | 1/10 | 0/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| FatigueGeneral disorders | 0/16 | 0/16 | 0/13 | 0/16 | 0/10 | 1/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| Vessel puncture site painGeneral disorders | 0/16 | 0/16 | 0/13 | 0/16 | 0/10 | 1/10 | 0/6 | 0/15 | 0/15 | 0/16 | 0/16 | 0/15 | 0/14 |
| Age, Continuous(Years) | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF | Total |
|---|---|---|---|---|
| Mean | 49.2 ± 14.10 | 47.8 ± 13.43 | 45.3 ± 12.22 | 47.5 ± 13.12 |
| Sex: Female, Male(Participants) | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF | Total |
|---|---|---|---|---|
| Female | 8 | 4 | 7 | 19 |
| Male | 11 | 6 | 9 | 26 |
| Race/Ethnicity, Customized(Participants) | MT-12hr Fasted/MT-8hr Fasted/IR Fasted/MT-12hr Fed (High Fat) | MT 120mg Fasted/MT 240mg Fasted/ MT 300mg Fed (Standard) | MM240 Fast/IR240 Fast/MM480 Fast/MM480 Fed/MM480 DF/MM240 DF | Total |
|---|---|---|---|---|
| Asian - East Asian Heritage | 1 | 0 | 1 | 2 |
| White - White/Caucasian/European Heritage | 18 | 10 | 14 | 42 |
| Asian - South East Asian Heritage | 0 | 0 | 1 | 1 |
PDFs hosted by the registry, ClinicalTrials.gov.
Plan to share: Yes — IPD for this study is available via the Clinical Study Data Request site
Supporting information: Study protocol, Statistical analysis plan, Informed consent form, Clinical study report
Time frame: IPD is available via the Clinical Study Data Request site (copy the URL below to your browser)
Access criteria: Access is provided after a research proposal is submitted and has received approval from the Independent Review Panel and after a Data Sharing Agreement is in place. Access is provided for an initial period of 12 months but an extension can be granted, when justified, for up to another 12 months.
Data sharing details ↗ · www.clinicalstudydatarequest.com
Ran from Sep 2017 to primary completion in Nov 2018, 13 months.
Results were first posted in Jan 2020, 1 year 1 month after primary completion.
Of 69 industry-sponsored phase 1 interventional studies under Autoimmune Diseases, half reached primary completion within 13 months of starting (the median), counting those still running; a quarter within 9 and three quarters within 32. This study's 13 months is close to that.
Counting every sponsor, half of 95 studies reached it within 23 months; a quarter within 9 and three quarters within 36.
How these figures are worked out, and which studies are left out of them.
This study is completed, as verified in Aug 2021. You cannot join it, but the record below documents what was studied.
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Studies of the drug tested here: GSK2982772