A Comparative Bioavailability Study of Lomitapide 20 mg Intact vs Sprinkled

NCT02044419 | Completed Phase 1 Results

• 1 other identifier: AEGR-733-032
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

Brief Summary

To compare the relative bioavailability of lomitapide when administered by sprinkling the contents of a 20 mg capsule of lomitapide in applesauce or in mashed banana to a single oral intact capsule dose of 20 mg lomitapide in healthy subjects.

Conditions

Healthy

Keywords

Comparative; Bioavailability; lomitapide

Outcome Measures

Primary Outcomes (6)

• AUC0-t

  Area under the concentration-time curve from hour 0 to the last measurable concentration of lomitapide and its metabolites (M1\& M3).

  predose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post-dose

• Cmax

  Maximum observed concentration of lomitapide and its metabolites (M1\& M3).

  predose 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 of lomitapide and its metabolites (M1\& M3).

  predose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post-dose

• t1/2

  Terminal elimination half-life of lomitapide and its metabolites (M1\& M3).

  predose 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 plasma concentration vs time curve from zero to infinity of lomitapide and its metabolites (M1\& M3).

  predose 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 of lomitapide and its metabolites (M1\& M3).

  predose and 1, 2, 3, 4, 5, 6, 8, 10, 12, 18, 24, 48, 72, 96, 120, 144, and 168 hours post-dose

Study Arms (3)

lomitapide sprinkled in applesauce

EXPERIMENTAL

Contents of single 20 mg capsule of lomitapide sprinkled in applesauce

Drug: lomitapide

lomitapide sprinkled in mashed banana

EXPERIMENTAL

Contents of single 20 mg capsule of lomitapide sprinkled in mashed banana

Drug: lomitapide

lomitapide (intact)

EXPERIMENTAL

Intact capsule of 20 mg lomitapide

Drug: lomitapide

Interventions

lomitapide DRUG

Also known as: Juxtapid, Lojuxta

lomitapide (intact); lomitapide sprinkled in applesauce; lomitapide sprinkled in mashed banana

Eligibility Criteria

• Age: 18 Years - 40 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Subject is a non-smoking healthy male or female, aged between 18 and 40 years of age.
• Subject has a BMI of 18.5 - 25 kg/m2.
• Subject has total body weight between \> 50 kg to ≤ 100 kg.
• Subjects must agree to use acceptable methods of contraception.
• All females, regardless of childbearing potential, must have a negative serum beta human chorionic gonadotropin pregnancy test at Screening and on admission.
• In good health, determined by no clinically significant or relevant abnormalities identified by a detailed medical history \& full physical examination.
• No known history of hypersensitivity or previous intolerance to lomitapide, applesauce, and/or banana.
• Subjects must be capable of understanding and complying with the requirements of the protocol and must have signed the informed consent form prior to undergoing any study-related procedures.

You may not qualify if:

• Subject has a clinically significant disease or any condition or disease that might affect drug absorption, distribution or excretion.
• History of stomach or intestinal surgery or resection that would potentially alter absorption and/or excretion of orally administered drugs.
• Any clinically significant abnormal laboratory, vital signs or other safety findings as determined by medical history, physical examination or other evaluations.
• History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance, unless approved by the Investigator;
• Electrocardiogram (ECG) abnormalities in the standard 12-lead ECG (at screening) such as a QTcF interval of \>450 msec, a history of a prolonged QTc interval or Brugada syndrome.
• History or current evidence of any clinically relevant cardiovascular, pulmonary, hepatic, renal, gastrointestinal, haematological, endocrinological, allergic, dermatological, metabolic, neurological, psychiatric or other disease.
• History or laboratory evidence of Gilbert's syndrome.
• Positive results in any of the serology tests for Hepatitis B Surface Antigen (HbsAg), anti-Hepatitis core antibody (anti-HBc Ig G \[and anti-HBc IgM if IgG is positive\], Hepatitis C antibodies (anti-HCV), and HIV 1 and 2 antibodies, (anti-HIV 1/2).
• Use of any drugs of abuse within 6 months prior to admission.
• Confirmed positive results from urine drug screen (amphetamines, benzodiazepines, cocaine, cannabinoids, opiates, barbiturates and methadone) or from the alcohol breath test at screening and on admission (Day -1).
• History or clinical evidence of alcohol or drug abuse within one year prior to admission.
• Mentally handicapped.
• Participation in a drug trial within 90 days prior to first drug administration.
• Use of any prescription medication within 2 weeks prior to admission (Day -1), with the exception of the oral contraceptive pill.
• Use of any substance inducing or inhibiting CYP3A4 enzymes within 30 days prior to admission (Day -1).

Sponsors & Collaborators

• Aegerion Pharmaceuticals, Inc.: lead

Study Sites (1)

Richmond Pharmacology Ltd

Croydon, Surrey, CR7 7YE, United Kingdom

Location

MeSH Terms

Interventions

BMS201038

Results Point of Contact

• Title: Alison Long, MD - VP Clinical
• Organization: Aegerion Pharmaceuticals, Inc.

alison.long@aegerion.com

857-242-5142

Study Officials

• Mark Sumeray, MD

  Aegerion Pharmaceuticals, Inc.

  STUDY CHAIR

• Ulrike Lorch, MD

  Richmond Phamacology, LTD

  PRINCIPAL INVESTIGATOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 6, 2013
• First Posted: January 24, 2014
• Study Start: October 30, 2013
• Primary Completion: December 23, 2013
• Study Completion: December 23, 2013
• Last Updated: February 13, 2018
• Results First Posted: February 13, 2018

Record last verified: 2018-02

Locations

GB (1)