Bioequivalence and Food Effect Bioavailability Study of Lumacaftor Film-Coated Tablets

NCT05968612 | Completed Phase 1

• 1 other identifier: QP586-01
• Study Type: interventional
• Target: 39
• Locations: 1 country
• Sites: 1

Brief Summary

The objective of this study is to assess bioequivalence of lumacaftor from Lumacaftor 200 mg Film-Coated Tablet Formulation (Qanatpharma) versus the reference commercial product, Lumacaftor 200 mg /Ivacaftor 125 mg Combination Film-Coated Tablet (Orkambi®) in the fed state, and food-effect bioavailability of Lumacaftor 200 mg Film-Coated Tablet Formulation (Qanatpharma) in the fasted and fed state in healthy, non-smoking, male and non-pregnant female volunteers, 18 to 55 years of age, inclusive.

Conditions

Healthy Volunteer

Keywords

lumacaftor; cystic fibrosis transmembrane regulator-corrector; CFTR-corrector; food effect; healthy volunteers; cerebral blood flow; CBF

Outcome Measures

Primary Outcomes (4)

• The maximal observed plasma concentration (Cmax)

  Serial blood samples for determination of study drug will be collected pre-dose at 0, and post-dose at 0.25, 0.5, 0.75, 1, 2, 3, 4, 5, 6, 7, 8, 9, 12, 24, 48, and 72 hours

  Up to 72 hours post dose in each treatment period

• Area under the concentration-time curve from time zero to 72 hours (AUC72)

  Serial blood samples for determination of study drug will be collected pre-dose at 0, and post-dose at 0.25, 0.5, 0.75, 1, 2, 3, 4, 5, 6, 7, 8, 9, 12, 24, 48, and 72 hours

  Up to 72 hours post dose in each treatment period

• Area under the concentration-time curve from time zero to infinity (AUCinf)

  Serial blood samples for determination of study drug will be collected pre-dose at 0, and post-dose at 0.25, 0.5, 0.75, 1, 2, 3, 4, 5, 6, 7, 8, 9, 12, 24, 48, and 72 hours

  Up to 72 hours post dose in each treatment period

• Time when the maximal plasma concentration is observed (Tmax)

  Serial blood samples for determination of study drug will be collected pre-dose at 0, and post-dose at 0.25, 0.5, 0.75, 1, 2, 3, 4, 5, 6, 7, 8, 9, 12, 24, 48, and 72 hours

  Up to 72 hours post dose in each treatment period

Study Arms (3)

Treatment A (Test-Fed)

EXPERIMENTAL

Following a 10-hour overnight fasting period, subjects will eat a high-fat, high-calorie breakfast, and 30 minutes later subjects will receive a single dose of 2 Lumacaftor 200 mg Film-Coated Tablets.

Drug: Lumacaftor 200 mg Film-Coated Tablet Formulation

Treatment B (Reference-Fed)

ACTIVE COMPARATOR

Following a 10-hour overnight fasting period, subjects will eat a high-fat, high-calorie breakfast, and 30 minutes later subjects will receive a single dose of 2 Lumacaftor 200 mg/Ivacaftor 125 mg Combination Film-Coated Tablets (Orkambi®)

Drug: Lumacaftor 200 mg/Ivacaftor 125 mg Film-Coated Tablet

Treatment C (Test-Fasted)

EXPERIMENTAL

Following a 10-hour overnight fasting period, subjects will receive a single dose of 2 Lumacaftor 200 mg Film-Coated Tablets.

Drug: Lumacaftor 200 mg Film-Coated Tablet Formulation

Interventions

Lumacaftor 200 mg/Ivacaftor 125 mg Film-Coated Tablet DRUG

Film-coated tablet administered orally.

Treatment B (Reference-Fed)

Lumacaftor 200 mg Film-Coated Tablet Formulation DRUG

Film-coated tablet administered orally.

Treatment A (Test-Fed); Treatment C (Test-Fasted)

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy, non-smoking male and non-pregnant female volunteers, 18 years to 55 years of age, inclusive.
• Body mass index (BMI) that is between 18.5 and 30.0 kg/m\^2, inclusive.
• Results of clinical laboratory tests are within the normal range or with a deviation that is not considered clinically significant by the principal investigator.
• Ability to fast for at least 10 hours and consume a high-fat, high-calorie meal, as well as standard meals.
• Agree not to have a tattoo or body piercing until the end of the study.
• Agree not to receive the COVID-19 vaccination from 7 days prior to the first study drug dose until 7 days after the last study drug administration in the study.
• Female subjects of childbearing potential and males who are able to father children must meet the criteria defined in the protocol.

You may not qualify if:

• Known history or presence of any clinically significant diseases or conditions unless determined as not clinically significant by the Investigator.
• Presence of any clinically significant illness within 30 days prior to first dosing, as determined by the Investigator.
• Presence of any significant physical or organ abnormality as determined by the Investigator.
• A positive test result for any of the following: HIV, Hepatitis B surface antigen, Hepatitis C, drugs of abuse (marijuana, amphetamines, barbiturates, cocaine, opiates, phencyclidine and benzodiazepines), alcohol breath test and cotinine. Positive pregnancy test for female subjects.
• Known history or presence of:
• Alcohol abuse or dependence within one year prior to first drug administration;
• Drug abuse or dependence;
• Hypersensitivity or idiosyncratic reaction to lumacaftor and ivacaftor, its excipients, and/or related substances;
• Food allergies
• Presence of any dietary restrictions unless deemed by the Investigator as "Not Clinically Significant".
• Severe allergic reactions (e.g. anaphylactic reactions, angioedema).
• Intolerance to and/or difficulty with blood sampling through venipuncture.
• Abnormal diet patterns (for any reason) during the four weeks preceding the study, including fasting, high protein diets, etc.
• Individuals who have donated, in the days prior to first study drug administration:
• mL of blood in the previous 30 days;

Sponsors & Collaborators

• Qanatpharma Canada LTD: lead

Study Sites (1)

BioPharma Services Inc.

Toronto, Ontario, M9L3A2, Canada

Location

Related Publications (1)

• Papaelias A, Lidington D, Bolz SS. Demonstrating Bioequivalence for a Lumacaftor Monosubstance Formulation Versus Orkambi(R) (Lumacaftor/Ivacaftor) in Healthy Subjects. Drugs R D. 2025 Sep;25(3):221-229. doi: 10.1007/s40268-025-00514-9. Epub 2025 Jun 23.

  PMID: 40551045 DERIVED

MeSH Terms

Interventions

lumacaftor; ivacaftor

Study Officials

• Isabella Szeto, MD, CCFP

  BioPharma Service Inc.

  PRINCIPAL INVESTIGATOR

Study Design

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

Study Record Dates

• First Submitted: July 21, 2023
• First Posted: August 1, 2023
• Study Start: November 17, 2023
• Primary Completion: December 18, 2023
• Study Completion: December 18, 2023
• Last Updated: December 26, 2023

Record last verified: 2023-12

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL
• Time Frame: 12 months after article publication and for up to 36 months following article publication
• Access Criteria: Data sharing requests can be made by qualified researchers for approved proposals under the terms of a Data Use Agreement.

Locations

CA (1)