A Study to Compare the Relative Bioavailability of Brigatinib When Swallowed as a Solution Versus When Swallowed as a Tablet in Healthy Adults

Phase 1

Completed

• Conditions: Healthy Volunteers
• Interventions: Drug: Brigatinib

• Registration Number: NCT06132867
• Lead Sponsor: Takeda

Brief Summary

The main aim of this study is to compare the amount of brigatinib in the blood of healthy adults after they have swallowed one dose either as a solution or as a tablet.

Detailed Description

The drug being tested in this study is called brigatinib. Brigatinib is being tested to assess its relative bioavailability when administered as an oral solution versus as an immediate-release tablet in healthy participants.

The study will enroll approximately 12 participants. Participants will be randomly assigned to one of the treatment sequences:

* Sequence 1: Treatment A followed by Treatment B

* Sequence 2: Treatment B followed by Treatment A wherein Treatment A is a 90 mg oral solution dose and Treatment B is a 90 mg tablet dose.

There will be a washout period of at least 14 days between brigatinib administration in each study period. The follow-up contact will occur 14 (±2) days post the last dose of study drug.

This single-center trial will be conducted in the United States. The overall study duration is approximately 56 days.

Study Timeline

• Study First Submitted: 2023-11-10
• Study First Submitted QC: 2023-11-10
• Study First Posted: 2023-11-15
• Study Start: 2023-12-20
• Primary Completion: 2024-02-17
• Study Completion: 2024-02-17
• Status Verified: 2024-12
• Results First Submitted: 2024-12-20
• Results First Submitted QC: 2024-12-20
• Last Update Submitted: 2024-12-20
• Results First Posted: 2025-01-23
• Last Update Posted: 2025-01-23

Recruitment & Eligibility

• Status: COMPLETED
• Sex: All
• Target Recruitment: 12

Inclusion Criteria

1. Continuous nonsmoker who has not used nicotine-containing products for at least 3 months prior to the first dosing and throughout the study.
2. Body mass index (BMI) ≥18.0 and ˂32.0 kilograms per meters squared (kg/m^2) at screening.
3. Pulse rate between 60 and 100 beats per minute (bpm) and a blood pressure between 90 to 140 millimeters of mercury (mmHg) systolic and 40 to 90 mmHg diastolic at screening and prior to dosing of Period 1.
4. Creatine phosphokinase is ≤1.1x upper limit of normal [ULN]; lipase, amylase, alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin, glucose, and activated partial thromboplastin time (aPTT) are ≤ULN at screening and check-in of Period 1.

Exclusion Criteria

1. Any history of major surgery.
2. History or presence of hypersensitivity or idiosyncratic reaction to the study drug or related compounds.
3. Unable to refrain from or anticipates the use of any drug, including prescription and nonprescription medications, herbal remedies, or vitamin supplements within 28 days prior to the first dosing and throughout the study.
4. Positive results at screening for Human Immunodeficiency Virus (HIV), Hepatitis B surface Antigen (HBsAg), or Hepatitis C Virus (HCV).
5. Positive coronavirus disease 2019 (COVID-19) results at first check-in.
6. Donation of blood or significant blood loss within 56 days prior to the first dosing.
7. Plasma donation within 7 days prior to the first dosing.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Sequence AB	Brigatinib	Participants received single dose of brigatinib 90 milligram (mg) as an oral solution in a fasted state on Day 1 of Period 1 (Treatment A) followed by single dose of brigatinib 90 mg as an immediate-release tablet in a fasted state on Day 1 of Period 2 (Treatment B). A washout period of at least 14 days was maintained between brigatinib administration in Period 1 and 2.
Sequence BA	Brigatinib	Participants received single dose of brigatinib 90 mg as an immediate-release tablet in a fasted state on Day 1 of Period 1 (Treatment B) followed by single dose of brigatinib 90 mg as an oral solution in a fasted state on Day 1 of Period 2 (Treatment A). A washout period of at least 14 days was maintained between brigatinib administration in Period 1 and 2.

Primary Outcome Measures

Name	Time	Method
Cmax: Maximum Observed Plasma Concentration for Brigatinib	Pre-dose, 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 120 and 168 hours post-dose
AUClast: Area Under the Plasma Concentration-Time Curve From Time Zero to the Time of the Last Quantifiable Concentration for Brigatinib	Pre-dose, 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 120 and 168 hours post-dose
AUCinf: Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity for Brigatinib	Pre-dose, 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 72, 120 and 168 hours post-dose

Secondary Outcome Measures

Name	Time	Method
Number of Participants With at Least One Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)	From first dose of the study drug up to Day 31	An adverse event (AE) was defined as any untoward medical occurrence in a clinical investigation participant who had signed informed consent form (ICF) to participate in a study. An AE can be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A TEAE was defined as an adverse event that was starting or worsening at the time of or after the first dose of brigatinib administered in the study. An SAE was defined as any untoward medical occurrence that at any dose resulted in death, was life threatening, requires inpatient hospitalization or prolongation of existing hospitalization, resulted in persistent or significant disability/incapacity, was a congenital anomaly or is an important medical event.

Trial Locations

Locations (1)

Celerion, Inc.; 🇺🇸 Tempe, Arizona, United States