Evaluation of the Relative Bioavailability of Bosutinib Capsules Under Fed Condition and Estimation of Food Effect on Orally Administered Bosutinib Capsule

• Sponsor: Pfizer (Industry)
• Overall Status: Completed
• CT.gov ID: NCT05032690
• Collaborator: (none)
• Enrollment: 32
• Location: 1
• Arms: 4
• Actual Duration (Months): 5.2
• Patients Per Site Per Month: 6.2

Study Details

Study Description

Brief Summary

This study is intended to estimate the bioavailability of a single 100 mg bosutinib capsules relative to four 25 mg capsules under fed condition in adult healthy participants and to estimate the effect of a high-fat, high-calorie meal on the bioavailability of a single 100 mg capsule of bosutinib relative to fasted condition in adults healthy participants. The comparisons will be performed using the pharmacokinetic parameters that define the rate and extend of absorption (Cmax, AUC). Statistical analyses will be performed after the administration of a single 100 mg dose under fed condition as the Reference treatment and the four 25 mg capsules as the Test treatment for the first comparison, and after administration of a single 100 mg dose under fasted condition as the Reference treatment and the 100 mg capsule under fed condition as the Test treatment for the second comparison.

Condition or Disease	Intervention/Treatment	Phase
Healthy Participants	Drug: Bosutinib capsule; Drug: Bosutinib capsule; Drug: Bosutinib; Drug: Bosutinib capsule	Phase 1

Study Design

• Study Type: Interventional
• Actual Enrollment: 32 participants
• Allocation: Randomized
• Intervention Model: Crossover Assignment
• Intervention Model Description: A Phase 1, open-label, randomized, single dose, 3-period, 4 sequence, crossover study in healthy participantsA Phase 1, open-label, randomized, single dose, 3-period, 4 sequence, crossover study in healthy participants
• Masking: None (Open Label)
• Primary Purpose: Basic Science
• Official Title: A PHASE 1, RANDOMIZED, OPEN-LABEL, 3-PERIOD, 4-SEQUENCE, CROSSOVER, SINGLE-DOSE STUDY TO COMPARE THE BIOAVAILABILITY OF ORALLY ADMINISTERED BOSUTINIB CAPSULES AND TO ESTIMATE THE EFFECT OF FOOD ON BOSUTINIB CAPSULE
• Actual Study Start Date: Jan 19, 2022
• Actual Primary Completion Date: Jun 25, 2022
• Actual Study Completion Date: Jun 25, 2022

Arms and Interventions

Arm	Intervention/Treatment
Experimental: Treatment B: Bosutinib four 25 mg capsule after meal Bosutinib four 25 mg capsule taken after a high-fat and high-calorie breakfast for comparison 1	Drug: Bosutinib capsule; Bosutinib four 25 mg capsule taken after a high-fat and high calorie breakfast
Active Comparator: Treatment A: Bosutinib 100 mg capsule after meal (active comparator) Bosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast for comparison 1	Drug: Bosutinib capsule; Bosutinib 100 mg capsule taken after a high-fat and high calorie breakfast
Experimental: Treatment A: Bosutinib 100 mg capsule after meal (experimental) Bosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast for comparison 2	Drug: Bosutinib capsule; Bosutinib 100 mg capsule taken after a high-fat and high-calorie breakfast
Active Comparator: Treatment C: Bosutinib 100 mg capsule after fasting Bosutinib 100 mg capsule taken after an overnight fast of at least 10 hours for comparison 2	Drug: Bosutinib; Bosutinib 100 mg capsule taken after an overnight fast of at least 10 hours

Outcome Measures

Primary Outcome Measures

1. Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0-inf)] [6 days]

2. Cmax [6 days]

Secondary Outcome Measures

1. Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) [6 days]

2. Time to Cmax (Tmax) [6 days]

3. Apparent Oral Clearance (CL/F) [6 days]

4. Apparent Volume of Distribution (Vz/F) [6 days]

5. Plasma elimination half-life (t1/2) [6 days]

Eligibility Criteria

Criteria

• Ages Eligible for Study: 18 Years to 55 Years
• Sexes Eligible for Study: All
• Accepts Healthy Volunteers: Yes

Inclusion Criteria:

• Female participants of non-childbearing potential and/or male participants must be 18 to 55 years of age, inclusive, at the time of signing the informed consent document (ICD)

• participants who are overtly healthy as determined by medical evaluation including a detailed medical history, complete physical examination, vital signs which include BP and pulse rate measurement, clinical laboratory tests, and electrocardiogram (ECG).

• Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures

Exclusion Criteria:

• Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, dermatological, or allergic disease.

• Any condition possibly affecting drug absorption (eg, gastrectomy, cholecystectomy).

• History of human immunodeficiency virus (HIV) infection, hepatitis B, or hepatitis C; positive testing for HIV, HBsAg,hepatitis B surface antigen (HBcAb) or hepatitis C antibody (HCVAb).

• Participants with ANY of the following abnormalities in clinical laboratory tests at screening, as assessed by the study-specific laboratory and confirmed by a single repeat test, if deemed necessary:

• estimated glomerular filtration rate (eGFR) (Chronic Kidney Disease Epidemiology Collaboration [CKD-EPI]) <90 mL/min/1.73 m2;

• aspartate aminotransferase (AST) or alanine aminotransferase (ALT) level >upper limit of normal (ULN);

• Serum (total and direct) bilirubin level > ULN; participants with a history of Gilbert's syndrome may have direct bilirubin measured and would be eligible for this study provided the direct bilirubin level is <= ULN;

• Amylase and lipase level > ULN.

Contacts and Locations

Locations

	Site	City	State	Country	Postal Code
1	Brussels Clinical Research Unit	Brussels	Bruxelles-capitale, Région DE	Belgium	B-1070

Sponsors and Collaborators

• Pfizer

Investigators

• Study Director: Pfizer CT.gov Call Center, Pfizer

Study Documents (Full-Text)

None provided.

More Information

Additional Information:

• To obtain contact information for a study center near you, click here.

Publications

None provided.

• Responsible Party: Pfizer
• ClinicalTrials.gov Identifier: NCT05032690
• Other Study ID Numbers: B1871062; 2021-004911-24
• First Posted: Sep 2, 2021
• Last Update Posted: Jul 8, 2022
• Last Verified: Jul 1, 2022

• Individual Participant Data (IPD) Sharing Statement: No
• Plan to Share IPD: No
• Studies a U.S. FDA-regulated Drug Product: Yes
• Studies a U.S. FDA-regulated Device Product: No
• Keywords provided by Pfizer: Bioavailability; Food Effect; Bosutinib; Maximum Observed Plasma Concentration (Cmax); Area Under the Curve (AUC)

Study Results

No Results Posted as of Jul 8, 2022