A Phase 1 interventional study of lomitapide in Intra-subject Variability of Pharmacokinetics, sponsored by Aegerion Pharmaceuticals, Inc.. Completed at 1 site in United Kingdom. Open to participants aged 18 Years to 40 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2020-03-11.
Sponsored by Aegerion Pharmaceuticals, Inc. (part of Chiesi Farmaceutici S.p.A.) · Phase 1, Interventional, and Other
Objectives:
To evaluate the intra-subject variability of the pharmacokinetics (PK) of single oral capsule doses of 20 mg lomitapide.
This study will be a single centre, open-label study. It will comprise of 2 single oral doses with at least a 14-day washout between doses. Following the first dose subjects will be discharged from the unit for the remainder of the washout period. Subjects will be re-admitted to the unit on Day -1 (Period 2) and following an overnight fast they will be administered the second dose on Day 1 (Period 2). Subjects will be discharged from the unit following the 168 h PK blood draw.
Aegerion Pharmaceuticals, Inc. is the lead sponsor of 17 studies on the registry; none are open to participants now.
First submitted before Aegerion Pharmaceuticals, Inc. became part of Chiesi Farmaceutici S.p.A..
Counted across the registry records on this site, refreshed daily.
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.
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.
An allergy, or another reaction of the immune system, to a substance. “Hypersensitivity to the study drug” means a known allergic reaction to it — not every side effect a medicine can have.
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.
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.
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.
CYP3A is a group of enzymes, mainly CYP3A4, in the liver and gut that break down many medicines. Some medicines, supplements and foods (grapefruit, St John’s wort) slow them down or speed them up, which changes how much of a study drug stays in the body.
Studies list them so they can be avoided or switched; bring a list of everything you take, including supplements.
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.
Hypersensitivity
An allergy, or another reaction of the immune system, to a substance. “Hypersensitivity to the study drug” means a known allergic reaction to it — not every side effect a medicine can have.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
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.
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.
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.
CYP3A (CYP3A4) inhibitors and inducers
CYP3A is a group of enzymes, mainly CYP3A4, in the liver and gut that break down many medicines. Some medicines, supplements and foods (grapefruit, St John’s wort) slow them down or speed them up, which changes how much of a study drug stays in the body.
Studies list them so they can be avoided or switched; bring a list of everything you take, including supplements.
Explained by clinicaltrials.gg, not part of the registry record. The study team decides who can take part.
It will comprise of 2 single oral doses with at least a 14-day washout between doses.
Drug: lomitapide
20 mg dose
Also known as: Juxtapid
Cmax
Maximum observed concentration of lomitapide and its metabolites, M1 \& M3.
Time frame: Pre dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post dose.
Tmax
Time to reach maximum plasma concentration
Time frame: Pre dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post dose.
AUC0-t
Area under the concentration-time curve from hour 0 to the last measurable concentration of lomitapide and its metabolites, M1 \& M3.
Time frame: Pre dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post dose.
AUC0-∞
Area under the concentration-time curve extrapolated to infinity for lomitapide and its metabolites, M1 \& M3.
Time frame: Pre dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post dose.
λz
Elimination rate constant estimated from individual linear regression of the terminal part of the log concentration vs time curve
Time frame: Pre dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post dose.
t1/2
Apparent terminal elimination half-life
Time frame: Pre dose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post dose.
| Milestone | Lomitapide |
|---|---|
| Started | 15 |
| Completed | 14 |
| Not completed | 1 |
| Withdrew: Withdrawal by subject | 1 |
| Milestone | Lomitapide |
|---|---|
| Started | 14 |
| Completed | 13 |
| Not completed | 1 |
| Withdrew: Withdrawal by subject | 1 |
Maximum observed concentration of lomitapide and its metabolites, M1 \& M3.
| ng/mL | PK of Lomitapide | PK of M1 | PK of M3 |
|---|---|---|---|
| Period 1 | 0.961 ± 0.556 | 2.34 ± 0.593 | 23.6 ± 7.08 |
| Period 2 | 1.02 ± 0.843 | 2.20 ± 0.664 | 22.8 ± 9.33 |
Time to reach maximum plasma concentration
| hr | PK of Lomitapide | PK of M1 | PK of M3 |
|---|---|---|---|
| Period 1 | 4.0 (1.00 to 18.0) | 5.00 (3.00 to 10.0) | 3.00 (1.00 to 4.03) |
| Period 2 | 5.00 (3.00 to 18.0) | 5.00 (2.00 to 6.00) | 3.00 (1.00 to 4.00) |
Area under the concentration-time curve from hour 0 to the last measurable concentration of lomitapide and its metabolites, M1 \& M3.
| ng*hr/mL | PK of Lomitapide | PK of M1 | PK of M3 |
|---|---|---|---|
| Period 1 | 40.2 ± 18.1 | 65.8 ± 22.7 | 319 ± 153 |
| Period 2 | 44.0 ± 21.7 | 62.8 ± 23.3 | 319 ± 176 |
Area under the concentration-time curve extrapolated to infinity for lomitapide and its metabolites, M1 \& M3.
| ng*hr/mL | PK of Lomitapide | PK of M1 | PK of M3 |
|---|---|---|---|
| Period 1 | 44.4 ± 19.9 | 68.3 ± 23.6 | 330 ± 158 |
| Period 2 | 48.3 ± 23.4 | 65.3 ± 24.1 | 330 ± 181 |
Elimination rate constant estimated from individual linear regression of the terminal part of the log concentration vs time curve
| 1/hr | PK of Lomitapide | PK of M1 | PK of M3 |
|---|---|---|---|
| Period 1 | 0.0141 ± 0.00196 | 0.0200 ± 0.00754 | 0.0155 ± 0.00370 |
| Period 2 | 0.0146 ± 0.00139 | 0.0189 ± 0.00410 | 0.0172 ± 0.00272 |
Apparent terminal elimination half-life
| hr | PK of Lomitapide | PK of M1 | PK of M3 |
|---|---|---|---|
| Period 1 | 50.3 ± 7.56 | 38.3 ± 10.6 | 46.9 ± 10.4 |
| Period 2 | 47.8 ± 4.35 | 38.0 ± 6.61 | 41.2 ± 6.90 |
Non-serious events are listed at a 0% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Period 1 | 0/15 (0%) | 0/15 (0%) | 4/15 (26.7%) |
| Period 2 | 0/13 (0%) | 0/13 (0%) | 1/13 (7.7%) |
| Event | Period 1 | Period 2 |
|---|---|---|
| DiarrhoeaGastrointestinal disorders | 3/15 | 0/13 |
| NauseaGastrointestinal disorders | 2/15 | 0/13 |
| Abdominal DiscomfortGastrointestinal disorders | 2/15 | 1/13 |
| HeadacheNervous system disorders | 0/15 | 1/13 |
| Abdominal PainGastrointestinal disorders | 1/15 | 0/13 |
| FlatulenceGastrointestinal disorders | 1/15 | 0/13 |
| LymphdenopathyBlood and lymphatic system disorders | 1/15 | 0/13 |
| Upper Respiratory Tract InfectionInfections and infestations | 1/15 | 0/13 |
| Back PainMusculoskeletal and connective tissue disorders | 1/15 | 0/13 |
| AnxietyPsychiatric disorders | 1/15 | 0/13 |
| Age, Categorical(Participants) | Lomitapide |
|---|---|
| <=18 years | 0 |
| Between 18 and 65 years | 15 |
| >=65 years | 0 |
| Age, Continuous(years) | Lomitapide |
|---|---|
| Mean | 26.2 ± 4.9 |
| Sex: Female, Male(Participants) | Lomitapide |
|---|---|
| Female | 6 |
| Male | 9 |
| Region of Enrollment(participants) | Lomitapide |
|---|---|
| United Kingdom | 15 |
This study is completed, as verified in Feb 2020. You cannot join it, but the record below documents what was studied.
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Studies of the drug tested here: BMS201038
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