A Phase 1 interventional study of GSK2982772 capsule and Placebo capsule 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 2023-10-10.
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 14th 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 24th 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 62 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 |
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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.
This study is designed to evaluate the safety, tolerability and PK of GSK2982772, in repeat oral doses in healthy subjects. This study is being conducted to support administration of higher dose levels of GSK2982772 than initially studied in the First Time in Human (FTiH) study. This study will also assess the impact of food during the repeat doses of GSK2982772. This will be a two part study; Part A and Part B. Part A (cohort 1) - single ascending dose, randomized, placebo-controlled, 3-way crossover. Part B (cohorts 2, 3, 4 and 5) - repeat dose, randomized, placebo-controlled, sequential-group. Subjects will be randomized in 3:1 ratio to receive GSK2982772 or placebo in crossover manner on Day 1 of each of the three periods in Part A. Subjects will be randomized in 3:1 ratio to receive GSK2982772 or placebo in sequential groups for 14 days in cohort 2 of Part B and in 9:5 ratio to receive GSK2982772 or placebo in sequential groups for 14 days in cohorts 3, 4 and 5 of Part B. Approximately 66 subjects will be included in this study. The study duration, including screening and follow-up, will not be expected to exceed 13 weeks for Part A and 8 weeks for Part B.
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:
PART B Specific 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.
Able to have children. For women this usually means from the first period until menopause, unless permanently unable to through surgery; for men, unless permanently sterile. Read who the line is about — participants, women, men, or their partners.
Criteria about it usually ask for contraception during the study and for a time after it.
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.
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.
A recording of the heart’s electrical activity, taken with stickers on the chest, arms and legs. It takes a few minutes and does not hurt.
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.
Vaccines made with a weakened form of the germ, such as measles–mumps–rubella (MMR), chickenpox and yellow fever. They can be risky when the immune system is weakened. Flu injections are not live; the nasal flu spray is.
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.
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.
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.
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.
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.
Reproductive potential
Able to have children. For women this usually means from the first period until menopause, unless permanently unable to through surgery; for men, unless permanently sterile. Read who the line is about — participants, women, men, or their partners.
Criteria about it usually ask 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.
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.
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.
ECG (electrocardiogram)
A recording of the heart’s electrical activity, taken with stickers on the chest, arms and legs. It takes a few minutes and does not hurt.
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.
Live vaccines
Vaccines made with a weakened form of the germ, such as measles–mumps–rubella (MMR), chickenpox and yellow fever. They can be risky when the immune system is weakened. Flu injections are not live; the nasal flu spray is.
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.
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.
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.
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.
Eligible subjects will be randomized to receive treatment sequence ABC in Part A; A= GSK2982772 120 mg TID, B= GSK2982772 240 mg TID, and C= GSK2982772 360 mg BID. Subjects will receive oral capsule of GSK2982772 or placebo on Day 1 in each of the 3 treatment periods followed by a wash-out period of at least 7 days between dosing regimens.
Drug: GSK2982772 capsule · Drug: Placebo capsule
Eligible subjects will be randomized to receive treatment sequence ABP in Part A; A= GSK2982772 120 mg TID, B= GSK2982772 240 mg TID, and P= Placebo. Subjects will receive oral capsule of GSK2982772 or placebo on Day 1 in each of the 3 treatment periods followed by a wash-out period of at least 7 days between dosing regimens.
Drug: GSK2982772 capsule · Drug: Placebo capsule
Eligible subjects will be randomized to receive treatment sequence APC in Part A; A= GSK2982772 120 mg TID, P= Placebo and C= GSK2982772 360 mg BID. Subjects will receive oral capsule of GSK2982772 or placebo on Day 1 in each of the 3 treatment periods followed by a wash-out period of at least 7 days between dosing regimens.
Drug: GSK2982772 capsule · Drug: Placebo capsule
Eligible subjects will be randomized to receive treatment sequence PBC in Part A; P= Placebo, B= GSK2982772 240 mg TID and C= GSK2982772 360 mg BID. Subjects will receive oral capsule of GSK2982772 or placebo on Day 1 in each of the 3 treatment periods followed by a wash-out period of at least 7 days between dosing regimens.
Drug: GSK2982772 capsule · Drug: Placebo capsule
Eligible subjects will receive GSK2982772 oral capsule with a dose of 120 mg TID for 14 days in Part B.
Drug: GSK2982772 capsule
Eligible subjects will receive GSK2982772 oral capsule with a dose of 120 mg TID for 14 days in Part B.
Drug: GSK2982772 capsule
Eligible subjects will receive GSK2982772 oral capsule with a dose of 240 mg TID for 14 days in Part B.
Drug: GSK2982772 capsule
Eligible subjects will receive GSK2982772 oral capsule with a dose of 360 mg BID for 14 days in Part B.
Drug: GSK2982772 capsule
Subjects will receive placebo oral capsule for 14 days in Part B.
Drug: Placebo capsule
Subjects will receive placebo oral capsule for 14 days in Part B.
Drug: Placebo capsule
Subjects will receive placebo oral capsule for 14 days in Part B.
Drug: Placebo capsule
Subjects will receive placebo oral capsule for 14 days in Part B.
Drug: Placebo capsule
GSK2982772 will be available as size 00, white, opaque capsule containing white to almost white Solid (120 mg maximum fill per capsule). It will be administered orally with water to receive total dose of 120 mg, 240 mg or 360 mg per randomization.
Placebo will be available as size 00, white, opaque capsule containing white to almost white Solid. It will be administered orally with water.
Number of Subjects With Adverse Events (AEs) and Serious AEs (SAEs): Part A
An AE is any untoward medical occurrence in a clinical study subjects, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment will be categorized as SAE.
Time frame: Up to Day 14
Number of Participants With AEs and SAEs: Part B
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment were categorized as SAE.
Time frame: Up to Day 28
Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part A
Blood samples were collected from participants for the analysis of following clinical chemistry parameters: alanine amino transferase (ALT), albumin, alkaline phosphatase, aspartate amino transferase (AST), calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times Upper Limit of Normal (ULN) units per liter (U/L) for ALT, \<30 grams per liter (g/L) for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 millimoles per liter (mmol/L) for calcium, \>44.2 micromoles per liter (µmol/L) for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 9
Number of Participants With Worst Case Clinical Chemistry Parameters by Potential Clinical Importance Criteria: Part B
Blood samples were collected from participants for the analysis of following clinical chemistry parameters: ALT, albumin, alkaline phosphatase, AST, calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times ULN U/L for ALT, \<30 g/L for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 mmol/L for calcium, \>44.2 µmol/L for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 4
Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part A
Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and white blood cell (WBC) counts. PCI ranges were \>0.54 or \< 0.075 proportion of red blood cells (RBC) in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 9
Number of Participants With Worst Case Hematology Parameters by Potential Clinical Importance Criteria: Part B
Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and WBC counts. PCI ranges were \>0.54 or \< 0.075 proportion of RBC in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
Time frame: Up to Week 4
Number of Participants With Worst Case Urinalysis Results: Part A
Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented.
Time frame: Up to Week 9
Number of Participants With Worst Case Urinalysis Results: Part B
Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented.
Time frame: Up to Week 4
Number of Participants With Abnormal Vital Signs: Part A
Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 millimeters of mercury \[mmHg\]), diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported.
Time frame: Up to Week 9
Number of Participants With Abnormal Vital Signs: Part B
Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 mmHg, diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported.
Time frame: Up to Week 4
Number of Participants With Abnormal Electrocardiogram (ECG) Findings: Part A
12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition.
Time frame: Up to Day 4
Number of Participants With Abnormal ECG Findings: Part B
12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition.
Time frame: Up to Week 4
Area Under the Concentration-time Curve (AUC) From Time Zero to 24 Hours (AUC[0-24]) Following TID Dosing of GSK2982772: Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20, 40minutes, 1 hour, 1hr 30min, 2, 3, 5, 7hour, 7hr 20min,and 7hr 40 min, 8hr, 8hr 30min, 9hr, 10hr, 12hr, 14hr, 14hr 20min, 14hr 40 min, 15hr, 15hr 30min, 16hr, 17hr, 19hr, 22hr, 24hours post dose on Day1
AUC(0-24) Following BID Dosing of GSK2982772: Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20min, 40min, 1hr, 1hr 30min, 2hr, 3hr, 4hr, 6hr, 8hr, 10hr, 12hr, 12hr 20min, 12hr 40min, 13hr, 13hr 30min, 14hr, 15hr, 16hr, 19hr, 22hr, 24hr post dose on Day 1.
AUC[0-24] Following TID Dosing of GSK2982772: Part B
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20, 40minutes, 1 hour, 1hr 30min, 2, 3, 5, 7hour, 7hr 20min,and 7hr 40 min, 8hr, 8hr 30min, 9hr, 10hr, 12hr, 14hr, 14hr 20min, 14hr 40 min, 15hr, 15hr 30min, 16hr, 17hr, 19hr, 22hr, 24hours post dose on Day14
AUC (0-7) Following TID Dosing of GSK2982772 : Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Day 1
AUC (7-14) Following TID Dosing of GSK2982772 : Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 1
AUC (14-24) Following TID Dosing of GSK2982772 : Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 hours ,15 hours 30 minutes, 16, 19, 22 and 24 hours on Day 1
AUC (0-12) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours,12 hours on Day 1
AUC (12-24) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours, 12 hours 20 and 40 minutes, 13 and 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours on Day 1
AUC(0-7) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 1 and 14
AUC (7-14) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 and 7 hours 20 and 40 minutes, 8 and 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 14
AUC (14-24) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 minutes, 14 hours 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours on Day 14
Maximum Observed Plasma Drug Concentration Cmax (0-7) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, and 7 hours post dose on Day 1
Cmax (7-14) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours, 7 hours 20 and 40 minutes, 8 and 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 1
Cmax (14-24) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 and 15 hours 30 minutes, 16, 19, 22 and 24 hours post dose on Day 1
Cmax (0-12) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours and 12 hours post dose on Day 1
Cmax (12-24) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours, 12 hours 20 and 40 minutes, 13 and 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours post dose on Day 1
Cmax (0-7) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours post dose on Days 1 and 14
Cmax (7-14) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours on Day 14
Cmax (14-24) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 14
Time to Cmax (Tmax) (0-7) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, and 7 hours post dose on Day 1
Tmax (7-14) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7hours, 7 hours 20 and 40 minutes, 8 hours, 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 1
Tmax (14-24) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours, 14 hours 20 and 40 minutes, 15 hours, 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 1
Tmax (0-12) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1hour, 1 hour 30 minutes, 2, 3, 4, 6, 8, 10 hours and 12 hours post dose on Day 1
Tmax (12-24) Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours, 12 hours 20 and 40 minutes, 13 hours, 13 hours 30 minutes, 14, 15, 16, 19, 22 and 24 hours post dose on Day 1
Tmax (0-7) Following TID Dosing of GSK2982772 Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 hour, 1 hour 30 minutes, 2, 3, 5, 7 hours post dose on Days 1 and 14
Tmax (7-14) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7hours and 7 hours 20 and 40 minutes, 8hours, 8 hours 30 minutes, 9, 10, 12, 14 hours post dose on Day 14
Tmax (14-24) Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14hours, 14 hours 20 and 40 minutes, 15 hours and 15 hours 30 minutes, 16, 17, 19, 22 and 24 hours post dose on Day 14
Observed Trough Plasma Drug Concentration at 7 Hour (C7),Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours post-dose on Day 1
Observed Trough Plasma Drug Concentration at 14 Hours (C14) Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours post-dose on Day 1
C24 Following TID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 24 hours post-dose on Day 1
C12 Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 12 hours post-dose on Day 1
C24 Following BID Dosing of GSK2982772 in Part A
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 24 hours post-dose on Day 1
C0 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose on Day 14
C7 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 7 hours post-dose on Days 1 and 14
C14 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 14 hours post-dose on Day 14
C24 Following TID Dosing of GSK2982772 in Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: 24 hours post-dose on Day 14
AUC([0-7] Following TID Dosing of GSK2982772 in Fed State of Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11
Cmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11
Tmax (0-7) Following TID Dosing of GSK2982772 in Fed State of Part B
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
Time frame: Pre-dose, 20 and 40 minutes, 1 and 1 hour 30 minutes, 2, 3, 5, 7 hours on Days 9 and 11
Ratio of Plasma 4 Beta-hydroxycholesterol to Cholesterol: Part B
Blood samples were collected into EDTA tubes and processed to plasma for 4 beta-hydroxycholesterol and cholesterol. Ratio of 4 beta-hydroxycholesterol to cholesterol is presented
Time frame: Pre-dose on Day 1 and 24 hours post first dose on Day 14
This study consisted of two parts; part A was single ascending dose, 3-way crossover and part B was repeat dose, sequential assignment which investigated the safety, tolerability, and pharmacokinetics of GSK2982772, in healthy participants.
| Milestone | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|---|---|---|---|
| Started | 3 | 3 | 3 | 3 | 0 | 0 | 0 | 0 |
| Completed | 3 | 2 | 3 | 3 | 0 | 0 | 0 | 0 |
| Not completed | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
| Withdrew: Adverse event | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
| Milestone | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|---|---|---|---|
| Started | 3 | 3 | 3 | 3 | 0 | 0 | 0 | 0 |
| Completed | 1 | 3 | 3 | 3 | 0 | 0 | 0 | 0 |
| Not completed | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Withdrew: Adverse event | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Withdrew: Physician decision | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Milestone | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|---|---|---|---|
| Started | 3 | 3 | 3 | 3 | 0 | 0 | 0 | 0 |
| Completed | 3 | 3 | 3 | 3 | 0 | 0 | 0 | 0 |
| Not completed | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Milestone | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|---|---|---|---|
| Started | 0 | 0 | 0 | 0 | 14 | 20 | 13 | 0 |
| Completed | 0 | 0 | 0 | 0 | 11 | 10 | 8 | 0 |
| Not completed | 0 | 0 | 0 | 0 | 3 | 10 | 5 | 0 |
| Withdrew: Adverse event | 0 | 0 | 0 | 0 | 1 | 2 | 4 | 0 |
| Withdrew: Physician decision | 0 | 0 | 0 | 0 | 2 | 8 | 1 | 0 |
An AE is any untoward medical occurrence in a clinical study subjects, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment will be categorized as SAE.
| Participants | Part A:Placebo | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID | Part A:GSK2982772 360 mg BID |
|---|---|---|---|---|
| AEs | 3 | 6 | 4 | 7 |
| SAEs | 0 | 0 | 0 | 0 |
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect or any other situation according to medical or scientific judgment were categorized as SAE.
| Participants | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|
| AEs | 9 | 17 | 12 | — |
| SAEs | 1 | 0 | 0 | — |
Blood samples were collected from participants for the analysis of following clinical chemistry parameters: alanine amino transferase (ALT), albumin, alkaline phosphatase, aspartate amino transferase (AST), calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times Upper Limit of Normal (ULN) units per liter (U/L) for ALT, \<30 grams per liter (g/L) for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 millimoles per liter (mmol/L) for calcium, \>44.2 micromoles per liter (µmol/L) for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
| Participants | Part A:Placebo | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID | Part A:GSK2982772 360 mg BID |
|---|---|---|---|---|
| ALT, Low | 0 | 0 | 0 | 0 |
| ALT, No change | 9 | 9 | 9 | 9 |
| ALT, High | 0 | 0 | 0 | 0 |
| Albumin, Low | 0 | 0 | 0 | 0 |
| Albumin, No change | 9 | 9 | 9 | 9 |
| Albumin, High | 0 | 0 | 0 | 0 |
| Alkaline phosphatase, Low | 0 | 0 | 0 | 0 |
| Alkaline phosphatase, No change | 9 | 9 | 9 | 9 |
| Alkaline phosphatase, High | 0 | 0 | 0 | 0 |
| AST, Low | 0 | 0 | 0 | 0 |
| AST, No change | 9 | 9 | 9 | 9 |
| AST, High | 0 | 0 | 0 | 0 |
| Calcium, Low | 0 | 0 | 0 | 0 |
| Calcium, No change | 9 | 9 | 9 | 9 |
| Calcium, High | 0 | 0 | 0 | 0 |
| Creatinine, Low | 0 | 0 | 0 | 0 |
| Creatinine, No change | 9 | 9 | 9 | 9 |
| Creatinine, High | 0 | 0 | 0 | 0 |
| Glucose, Low | 0 | 0 | 0 | 0 |
| Glucose, No change | 9 | 9 | 9 | 9 |
| Glucose, High | 0 | 0 | 0 | 0 |
| Potassium, Low | 0 | 0 | 0 | 0 |
| Potassium, No change | 9 | 9 | 9 | 9 |
| Potassium, High | 0 | 0 | 0 | 0 |
| Sodium, Low | 0 | 0 | 0 | 0 |
| Sodium, No change | 9 | 9 | 9 | 9 |
| Sodium, High | 0 | 0 | 0 | 0 |
| Total Bilirubin, Low | 0 | 0 | 0 | 0 |
| Total Bilirubin, No change | 9 | 9 | 9 | 9 |
| Total Bilirubin, High | 0 | 0 | 0 | 0 |
Blood samples were collected from participants for the analysis of following clinical chemistry parameters: ALT, albumin, alkaline phosphatase, AST, calcium, creatinine, glucose, potassium, sodium and total bilirubin. PCI ranges were \>=2 times ULN U/L for ALT, \<30 g/L for albumin, \>=2 times ULN U/L for alkaline phosphatase, \>=2 times ULN U/L for AST, \<2 or \>2.75 mmol/L for calcium, \>44.2 µmol/L for creatinine, \<3 or \>9 mmol/L for glucose, \<3 or \>5.5 mmol/L for potassium, \<130 or \>150 mmol/L for sodium and \>=1.5 times ULN for total bilirubin. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
| Participants | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|
| ALT, Low | 0 | 0 | 0 | — |
| ALT, No change | 14 | 19 | 13 | — |
| ALT, High | 0 | 1 | 0 | — |
| Albumin, Low | 0 | 0 | 0 | — |
| Albumin, No change | 14 | 20 | 13 | — |
| Albumin, High | 0 | 0 | 0 | — |
| Alkaline phosphatase, Low | 0 | 0 | 0 | — |
| Alkaline phosphatase, No change | 14 | 20 | 13 | — |
| Alkaline phosphatase, High | 0 | 0 | 0 | — |
| AST, Low | 0 | 0 | 0 | — |
| AST, No change | 14 | 19 | 13 | — |
| AST, High | 0 | 1 | 0 | — |
| Calcium, Low | 0 | 0 | 0 | — |
| Calcium, No change | 14 | 20 | 13 | — |
| Calcium, High | 0 | 0 | 0 | — |
| Creatinine, Low | 0 | 0 | 0 | — |
| Creatinine, No change | 14 | 20 | 13 | — |
| Creatinine, High | 0 | 0 | 0 | — |
| Glucose, Low | 0 | 0 | 0 | — |
| Glucose, No change | 14 | 20 | 13 | — |
| Glucose, High | 0 | 0 | 0 | — |
| Potassium, Low | 0 | 0 | 0 | — |
| Potassium, No change | 14 | 20 | 12 | — |
| Potassium, High | 0 | 0 | 1 | — |
| Sodium, Low | 0 | 0 | 0 | — |
| Sodium, No change | 14 | 20 | 13 | — |
| Sodium, High | 0 | 0 | 0 | — |
| Total Bilirubin, Low | 0 | 0 | 0 | — |
| Total Bilirubin, No change | 14 | 20 | 13 | — |
| Total Bilirubin, High | 0 | 0 | 0 | — |
Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and white blood cell (WBC) counts. PCI ranges were \>0.54 or \< 0.075 proportion of red blood cells (RBC) in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
| Participants | Part A:Placebo | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID | Part A:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Hematocrit, Low | 0 | 0 | 0 | 0 |
| Hematocrit, No change | 9 | 9 | 9 | 9 |
| Hematocrit, High | 0 | 0 | 0 | 0 |
| Hemoglobin, Low | 0 | 0 | 0 | 0 |
| Hemoglobin, No change | 9 | 9 | 9 | 9 |
| Hemoglobin, High | 0 | 0 | 0 | 0 |
| Lymphocytes, Low | 0 | 0 | 0 | 0 |
| Lymphocytes, No change | 9 | 9 | 9 | 9 |
| Lymphocytes, High | 0 | 0 | 0 | 0 |
| Platelet count, Low | 0 | 0 | 0 | 0 |
| Platelet, No change | 9 | 9 | 9 | 9 |
| Platelet, High | 0 | 0 | 0 | 0 |
| Total Neutrophils, Low | 1 | 0 | 0 | 0 |
| Total Neutrophils, No change | 8 | 9 | 9 | 9 |
| Total Neutrophils, High | 0 | 0 | 0 | 0 |
| WBC count, Low | 0 | 0 | 0 | 0 |
| WBC, No change | 9 | 9 | 9 | 9 |
| WBC, High | 0 | 0 | 0 | 0 |
Blood samples were collected from participants for analysis of following hematology parameters; hematocrit, hemoglobin, lymphocytes, platelet count, total neutrophils and WBC counts. PCI ranges were \>0.54 or \< 0.075 proportion of RBC in blood for hematocrit, \<25 or \>180 g/L for hemoglobin, 0.8 x10\^9 cells/L for lymphocytes, \<1.5 x10\^9 cells/L for neutrophils, \<100 or \>550 x10\^9 cells/L for platelets and \<3 or 20\> x 10\^9 cells per liter WBC. Participants were counted in the worst case category that their value changed to low, normal or high. If values were unchanged (example: High to High), or whose value became normal, were recorded in 'No Change' category.
| Participants | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Hematocrit, Low | 0 | 0 | 0 | — |
| Hematocrit, No change | 14 | 20 | 13 | — |
| Hematocrit, High | 0 | 0 | 0 | — |
| Hemoglobin, Low | 0 | 0 | 0 | — |
| Hemoglobin, No change | 14 | 20 | 13 | — |
| Hemoglobin, High | 0 | 0 | 0 | — |
| Lymphocytes, Low | 0 | 0 | 1 | — |
| Lymphocytes, No change | 14 | 20 | 12 | — |
| Lymphocytes, High | 0 | 0 | 0 | — |
| Platelet count, Low | 0 | 0 | 0 | — |
| Platelet, No change | 14 | 20 | 13 | — |
| Platelet, High | 0 | 0 | 0 | — |
| Total Neutrophils, Low | 0 | 1 | 3 | — |
| Total Neutrophils, No change | 14 | 19 | 10 | — |
| Total Neutrophils, High | 0 | 0 | 0 | — |
| WBC count, Low | 0 | 0 | 0 | — |
| WBC, No change | 14 | 20 | 13 | — |
| WBC, High | 0 | 0 | 0 | — |
Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented.
| Participants | Part A:Placebo | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID | Part A:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Cellular casts, No change | 3 | 1 | 1 | 1 |
| Cellular casts, Any increase | 0 | 0 | 0 | 0 |
| Cellular casts, Increase to 1-9/HPF | 0 | 0 | 0 | 0 |
| Cellular casts, Increase to 10-50/HPF | 0 | 0 | 0 | 0 |
| Granular casts, No change | 3 | 1 | 1 | 1 |
| Granular casts, Any increase | 0 | 0 | 0 | 0 |
| Granular casts, Increase 1-9/HPF | 0 | 0 | 0 | 0 |
| Granular casts, Increase 10-50/HPF | 0 | 0 | 0 | 0 |
| Hyaline casts, No change | 3 | 1 | 1 | 1 |
| Hyaline casts, Any increase | 0 | 0 | 0 | 0 |
| Hyaline casts, Increase 1-9/HPF | 0 | 0 | 0 | 0 |
| Hyaline casts, Increase 10-50/HPF | 0 | 0 | 0 | 0 |
| RBC, No change | 3 | 0 | 1 | 0 |
| RBC, Any increase | 0 | 1 | 0 | 1 |
| RBC, Increase 1-9/HPF | 0 | 1 | 0 | 1 |
| RBC, Increase 10-50/HPF | 0 | 0 | 0 | 0 |
| WBC, No change | 3 | 1 | 1 | 0 |
| WBC, Any increase | 0 | 0 | 0 | 1 |
| WBC, Increase 1-9/HPF | 0 | 0 | 0 | 1 |
| WBC, Increase 10-50/HPF | 0 | 0 | 0 | 0 |
Urine samples were collected from participants for analysis of following parameters: cellular casts, granular casts, hyaline casts, RBC and WBC and were counted as cells per high-power field (cells/HPF). The number of participants with cells in urine has been presented.
| Participants | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Cellular casts, No change | — | 7 | 2 | — |
| Cellular casts, Any increase | — | 0 | 0 | — |
| Cellular casts, Increase to 1-9/HPF | — | 0 | 0 | — |
| Cellular casts, Increase to 10-50/HPF | — | 0 | 0 | — |
| Granular casts, No change | — | 7 | 2 | — |
| Granular casts, Any increase | — | 0 | 0 | — |
| Granular casts, Increase 1-9/HPF | — | 0 | 0 | — |
| Granular casts, Increase 10-50/HPF | — | 0 | 0 | — |
| Hyaline casts, No change | — | 7 | 2 | — |
| Hyaline casts, Any increase | — | 0 | 0 | — |
| Hyaline casts, Increase 1-9/HPF | — | 0 | 0 | — |
| Hyaline casts, Increase 10-50/HPF | — | 0 | 0 | — |
| RBC, No change | — | 5 | 1 | — |
| RBC, Any increase | — | 2 | 1 | — |
| RBC, Increase 1-9/HPF | — | 2 | 1 | — |
| RBC, Increase 10-50/HPF | — | 0 | 0 | — |
| WBC, No change | — | 5 | 2 | — |
| WBC, Any increase | — | 2 | 0 | — |
| WBC, Increase 1-9/HPF | — | 2 | 0 | — |
| WBC, Increase 10-50/HPF | — | 0 | 0 | — |
Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 millimeters of mercury \[mmHg\]), diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported.
| Participants | Part A:Placebo | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID | Part A:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Number of Participants With Abnormal Vital Signs: Part A | 6 | 8 | 7 | 8 |
Vital signs were measured in a supine position after 5 minutes rest. The PCI criteria for vital signs included: systolic blood pressure \<85 and \>160 mmHg, diastolic blood pressure \<45 mmHg and \>100 mmHg, heart rate \<40 and \>100 beats per minute, body temperature \<=35.5 and \>=37.8 degrees Celsius and respiration rate \<=8 and \>=20 breaths per minute. Data of participants with potential clinical importance has been reported.
| Participants | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Number of Participants With Abnormal Vital Signs: Part B | 11 | 20 | 12 | — |
12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition.
| Participants | Part A:Placebo | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID | Part A:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Abnormal, not clinically significant | 1 | 0 | 2 | 4 |
| Abnormal, clinically significant | 0 | 0 | 0 | 0 |
12-lead ECG's were obtained in the supine position after 5 minutes of rest using an ECG machine that automatically calculated the heart rate and measured PR, QRS, QT and QT duration corrected for heart rate by Fridericia's formula (QTcF) intervals. Clinically significant and not clinically significant abnormal ECG findings have been presented. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition.
| Participants | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg BID |
|---|---|---|---|---|
| Abnormal, not clinically significant | 3 | 4 | 3 | — |
| Abnormal, clinically significant | 0 | 0 | 0 | — |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Area Under the Concentration-time Curve (AUC) From Time Zero to 24 Hours (AUC[0-24]) Following TID Dosing of GSK2982772: Part A | 21.22 ± 41.37 | 46.13 ± 37.38 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 360 mg BID |
|---|---|
| AUC(0-24) Following BID Dosing of GSK2982772: Part A | 54.02 ± 36.02 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| AUC[0-24] Following TID Dosing of GSK2982772: Part B | 25.67 ± 28.81 | 52.00 ± 45.26 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| AUC (0-7) Following TID Dosing of GSK2982772 : Part A | 6.053 ± 33.87 | 11.686 ± 33.50 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| AUC (7-14) Following TID Dosing of GSK2982772 : Part A | 7.829 ± 44.25 | 17.823 ± 42.11 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| AUC (14-24) Following TID Dosing of GSK2982772 : Part A | 7.213 ± 48.85 | 16.300 ± 39.72 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 360 mg BID |
|---|---|
| AUC (0-12) Following BID Dosing of GSK2982772 in Part A | 21.80 ± 24.41 |
Blood samples were collected at indicated timepoints for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part A:GSK2982772 360 mg BID |
|---|---|
| AUC (12-24) Following BID Dosing of GSK2982772 in Part A | 31.69 ± 48.02 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hour*microgram per millilter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| AUC (0-7), Day 1, n=20, 13 | 6.550 ± 37.67 | 11.895 ± 33.98 |
| AUC (0-7), Day 14, n=10, 9 | 7.485 ± 25.53 | 14.835 ± 45.30 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| AUC (7-14) Following TID Dosing of GSK2982772 in Part B | 9.095 ± 30.57 | 17.372 ± 34.96 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*microgram per millilter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| AUC (14-24) Following TID Dosing of GSK2982772 in Part B | 8.988 ± 33.57 | 19.816 ± 55.60 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Maximum Observed Plasma Drug Concentration Cmax (0-7) Following TID Dosing of GSK2982772 in Part A | 1.7672 ± 41.78 | 3.3125 ± 25.88 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Cmax (7-14) Following TID Dosing of GSK2982772 in Part A | 2.148 ± 36.24 | 5.007 ± 33.09 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Cmax (14-24) Following TID Dosing of GSK2982772 in Part A | 1.4156 ± 47.03 | 3.4812 ± 28.46 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 360 mg BID |
|---|---|
| Cmax (0-12) Following BID Dosing of GSK2982772 in Part A | 4.967 ± 30.75 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 360 mg BID |
|---|---|
| Cmax (12-24) Following BID Dosing of GSK2982772 in Part A | 6.965 ± 61.70 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Cmax (0-7), Day 1, n=20, 13 | 2.0883 ± 37.87 | 3.2333 ± 37.04 |
| Cmax (0-7), Day 14, n=10, 9 | 2.2239 ± 30.03 | 4.3784 ± 45.62 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Cmax (7-14) Following TID Dosing of GSK2982772 in Part B | 2.505 ± 26.70 | 5.435 ± 32.59 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per millilter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Cmax (14-24) Following TID Dosing of GSK2982772 in Part B | 1.9205 ± 30.82 | 4.1607 ± 38.79 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Time to Cmax (Tmax) (0-7) Following TID Dosing of GSK2982772 in Part A | 3.008 (2.00 to 5.02) | 2.043 (1.50 to 3.01) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Tmax (7-14) Following TID Dosing of GSK2982772 in Part A | 10.000 (8.00 to 12.00) | 9.000 (8.50 to 10.02) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Tmax (14-24) Following TID Dosing of GSK2982772 in Part A | 19.00 (16.0 to 22.0) | 17.02 (16.0 to 24.0) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part A:GSK2982772 360 mg BID |
|---|---|
| Tmax (0-12) Following BID Dosing of GSK2982772 in Part A | 3.000 (1.50 to 4.02) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part A:GSK2982772 360 mg BID |
|---|---|
| Tmax (12-24) Following BID Dosing of GSK2982772 in Part A | 14.01 (13.5 to 15.0) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Tmax (0-7), Day 1, n=20, 13 | 2.000 (1.00 to 3.01) | 3.000 (1.00 to 3.01) |
| Tmax (0-7), Day 14, n=10, 9 | 1.750 (1.00 to 3.03) | 2.003 (1.00 to 3.00) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Tmax (7-14) Following TID Dosing of GSK2982772 in Part B | 9.001 (8.50 to 10.00) | 10.008 (8.50 to 12.00) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Tmax (14-24) Following TID Dosing of GSK2982772 in Part B | 17.02 (15.0 to 19.0) | 18.92 (16.0 to 19.0) |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Observed Trough Plasma Drug Concentration at 7 Hour (C7),Following TID Dosing of GSK2982772 in Part A | 0.3614 ± 84.67 | 0.7723 ± 89.30 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| Observed Trough Plasma Drug Concentration at 14 Hours (C14) Following TID Dosing of GSK2982772 in Part A | 0.4318 ± 86.28 | 0.7487 ± 76.95 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part A:GSK2982772 120 mg TID | Part A:GSK2982772 240 mg TID |
|---|---|---|
| C24 Following TID Dosing of GSK2982772 in Part A | 0.34518 ± 82.34 | 0.59880 ± 158.88 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis. Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per millilter | Part A:GSK2982772 360 mg BID |
|---|---|
| C12 Following BID Dosing of GSK2982772 in Part A | 0.3490 ± 98.83 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per millililter | Part A:GSK2982772 360 mg BID |
|---|---|
| C24 Following BID Dosing of GSK2982772 in Part A | 0.36965 ± 101.70 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| C0 Following TID Dosing of GSK2982772 in Part B | 0.29926 ± 56.63 | 0.57528 ± 136.34 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| C7, Day 1, n=20, 13 | 0.3345 ± 50.78 | 0.6105 ± 57.01 |
| C7, Day 14, n=10, 9 | 0.3718 ± 43.85 | 0.6885 ± 75.98 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| C14 Following TID Dosing of GSK2982772 in Part B | 0.3830 ± 53.04 | 0.6912 ± 106.01 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| C24 Following TID Dosing of GSK2982772 in Part B | 0.22712 ± 60.78 | 0.33342 ± 180.82 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours*micrograms per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| AUC (0-7) following normal breakfast, Day 9 | 7.743 ± 31.46 | 14.691 ± 37.63 |
| AUC (0-7) following high fat breakfast, Day 11 | 6.874 ± 24.64 | 15.987 ± 42.86 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Microgram per milliliter | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Cmax(0-7), following Normal Breakfast, Day 9 | 2.0918 ± 21.74 | 3.9440 ± 33.82 |
| Cmax(0-7), following High Fat Breakfast, Day 11 | 1.8098 ± 29.77 | 4.1171 ± 58.36 |
Blood samples were collected at indicated time-points for pharmacokinetic analysis of GSK2982772.Pharmacokinetic parameters were calculated by standard non-compartmental analysis.
| Hours | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|
| Tmax(0-7), Day 9 | 3.000 (1.04 to 5.00) | 3.000 (2.00 to 5.03) |
| Tmax (0-7), Day 11 | 4.000 (1.50 to 5.00) | 3.000 (2.00 to 5.00) |
Blood samples were collected into EDTA tubes and processed to plasma for 4 beta-hydroxycholesterol and cholesterol. Ratio of 4 beta-hydroxycholesterol to cholesterol is presented
| Ratio | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID |
|---|---|---|---|
| Day 1, Pre-dose; n=0, 19, 12 | — | 0.000019 ± 0.0000064 | 0.000023 ± 0.0000099 |
| Day 14, 24 hour; n=1, 10, 9 | 0.000016 ± NA | 0.000021 ± 0.0000089 | 0.000024 ± 0.0000065 |
Collected over On-treatment SAEs and non serious AEs were collected from the start of study treatment up to Day 14 for Part A and up to Day 28 for Part B.. Non-serious events are listed at a 0% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Part A: Placebo | 0/9 (0%) | 0/9 (0%) | 3/9 (33.3%) |
| Part A:GSK2982772 120 mg TID | 0/9 (0%) | 0/9 (0%) | 6/9 (66.7%) |
| Part A: GSK2982772 240 mg TID | 0/9 (0%) | 0/9 (0%) | 4/9 (44.4%) |
| Part A: GSK2982772 360 mg BID | 0/9 (0%) | 0/9 (0%) | 7/9 (77.8%) |
| Part B:Placebo | 0/14 (0%) | 1/14 (7.1%) | 9/14 (64.3%) |
| Part B: GSK2982772 120 mg TID | 0/20 (0%) | 0/20 (0%) | 17/20 (85%) |
| Part B: GSK2982772 240 mg TID | 0/13 (0%) | 0/13 (0%) | 12/13 (92.3%) |
| Part B: GSK2982772 360 mg BID | — | — | — |
| Event | Part A: Placebo | Part A:GSK2982772 120 mg TID | Part A: GSK2982772 240 mg TID | Part A: GSK2982772 360 mg BID | Part B:Placebo | Part B: GSK2982772 120 mg TID | Part B: GSK2982772 240 mg TID | Part B: GSK2982772 360 mg BID |
|---|---|---|---|---|---|---|---|---|
| Cerebrovascular accidentNervous system disorders | 0/9 | 0/9 | 0/9 | 0/9 | 1/14 | 0/20 | 0/13 | — |
| Event | Part A: Placebo | Part A:GSK2982772 120 mg TID | Part A: GSK2982772 240 mg TID | Part A: GSK2982772 360 mg BID | Part B:Placebo | Part B: GSK2982772 120 mg TID | Part B: GSK2982772 240 mg TID | Part B: GSK2982772 360 mg BID |
|---|---|---|---|---|---|---|---|---|
| Dermatitis contactSkin and subcutaneous tissue disorders | 1/9 | 2/9 | 3/9 | 3/9 | 3/14 | 4/20 | 1/13 | — |
| FlatulenceGastrointestinal disorders | 1/9 | 0/9 | 2/9 | 0/9 | 0/14 | 0/20 | 0/13 | — |
| Ventricular tachycardiaCardiac disorders | 0/9 | 1/9 | 0/9 | 2/9 | 0/14 | 0/20 | 0/13 | — |
| Abnormal dreamsPsychiatric disorders | 0/9 | 0/9 | 0/9 | 2/9 | 0/14 | 4/20 | 1/13 | — |
| HeadacheNervous system disorders | 0/9 | 0/9 | 0/9 | 0/9 | 2/14 | 3/20 | 2/13 | — |
| DizzinessNervous system disorders | 0/9 | 0/9 | 0/9 | 0/9 | 1/14 | 1/20 | 2/13 | — |
| Catheter site bruiseGeneral disorders | 0/9 | 0/9 | 0/9 | 0/9 | 0/14 | 3/20 | 0/13 | — |
| FatigueGeneral disorders | 0/9 | 0/9 | 0/9 | 0/9 | 0/14 | 3/20 | 0/13 | — |
| NasopharyngitisInfections and infestations | 0/9 | 0/9 | 0/9 | 1/9 | 2/14 | 1/20 | 0/13 | — |
| Atrial tachycardiaCardiac disorders | 0/9 | 0/9 | 0/9 | 0/9 | 2/14 | 0/20 | 0/13 | — |
Participants were not enrolled into the GSK2982772 360 mg BID of Part B as one participant in the 360 mg BID dose level in Part A exceeded the maximum concentration (Cmax) stopping criteria.
| Age, Continuous(Years) | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg TID | Total |
|---|---|---|---|---|---|---|---|---|---|
| Mean | 36.2 ± 9.04 | 42.5 ± 9.95 | 59.0 ± 3.61 | 49.0 ± 10.00 | 39.1 ± 9.66 | 43.3 ± 10.87 | 38.6 ± 11.03 | — | 45.25 ± 9.16 |
| Sex: Female, Male(Participants) | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg TID | Total |
|---|---|---|---|---|---|---|---|---|---|
| Female | 2 | 2 | 1 | 0 | 0 | 0 | 0 | 0 | 5 |
| Male | 3 | 2 | 2 | 3 | 14 | 20 | 13 | 0 | 57 |
| Race/Ethnicity, Customized(Participants) | Part A:GSK2982772 120 mg TID/240 mg TID/360 mg BID | Part A:GSK2982772 120 mg TID/240 mg TID/Placebo | Part A:GSK2982772 120 mg TID/Placebo/GSK2982772 360 mg BID | Part A:Placebo/GSK2982772 240 mg TID/360 mg BID | Part B:Placebo | Part B:GSK2982772 120 mg TID | Part B:GSK2982772 240 mg TID | Part B:GSK2982772 360 mg TID | Total |
|---|---|---|---|---|---|---|---|---|---|
| Black or African American | 0 | 1 | 1 | 0 | 0 | 1 | 3 | — | 6 |
| Asian - East Asian Heritage | 0 | 0 | 0 | 0 | 1 | 0 | 0 | — | 1 |
| Asian - Japanese Heritage | 0 | 0 | 0 | 0 | 1 | 0 | 0 | — | 1 |
| White - White/Caucasian/European Herit | 5 | 3 | 2 | 3 | 12 | 19 | 10 | — | 54 |
PDFs hosted by the registry, ClinicalTrials.gov.
Plan to share: Yes — Qualified researchers may request access to anonymized individual patient-level data (IPD) and related study documents of the eligible studies via the Data Sharing Portal. Details on GSK's data sharing criteria can be found at: https://www.gsk.com/en-gb/innovation/trials/data-transparency/
Supporting information: Study protocol, Statistical analysis plan, Informed consent form, Clinical study report
Time frame: Anonymized IPD is made available within 6 months of publication of primary, key secondary and safety results for studies in product with approved indication(s) or terminated asset(s) across all indications.
Access criteria: Anonymized IPD is shared with researchers whose proposals are approved by an 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 may be granted, when justified, for up to 6 months.
Data sharing details ↗ · www.gsk.com
Ran from Oct 2017 to primary completion in Oct 2018, 12 months.
Results were first posted in Nov 2019, 1 year 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 12 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 Sep 2023. You cannot join it, but the record below documents what was studied.
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Studies of the drug tested here: GSK2982772