Bioavailability of Bosutinib Administered as Capsule Contents Mixed With Applesauce or Yogurt Relative to Intact Capsules Under Fed Condition

Pfizer

Status and phase: Completed; Phase 1

Conditions: Healthy Participants

Treatments: Drug: Bosutinib capsule

Study type: Interventional

Funder types: Industry

Identifiers

NCT04916769

B1871063

2021-000500-38 (EudraCT Number)

Details and patient eligibility

About

This study is intended to estimate the relative bioavailability of a single 500 mg dose of bosutinib when administered as capsule contents mixed with applesauce or yogurt to intact capsules under fed condition in adult healthy participants. The comparisons will be performed using the pharmacokinetic parameters that define the rate and extent of absorption, those are Cmax and AUC. Statistical analyses will be performed comparing these parameters calculated after administration of a single 500 mg dose with the intact capsule formulation (100 mg x 5) as the Reference treatment and the capsule contents mixed with applesauce or yogurt (100 mg x 5) as the Test treatments.

Enrollment: 18 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Female participants of non childbearing potential and/or male participants must be 18 to 54 years of age, inclusive, at the time of signing the informed consent document (ICD).
• Capable of giving signed informed consent as described in Appendix 1, which includes compliance with the requirements and restrictions listed in the ICD and in this protocol.

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.

• 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:

  1. estimated glomerular filtration rate (eGFR) (Chronic Kidney Disease Epidemiology Collaboration [CKD-EPI]) < 90 mL/min/1.73 m2;
  2. Aspartate aminotransferase (AST) or alanine aminotransferase (ALT) level > upper limit of normal (ULN);
  3. 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;
  4. Amylase and lipase levels > ULN.

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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18 participants in 3 patient groups

Bosutinib capsule contents mixed with applesauce

Experimental group

Description:

Bosutinib capsule contents mixed with applesauce to healthy participants

Treatment:

Drug: Bosutinib capsule

Drug: Bosutinib capsule

Drug: Bosutinib capsule

Bosutinib capsule contents mixed with yogurt

Experimental group

Description:

Bosutinib capsule contents mixed with yogurt to healthy participants

Treatment:

Drug: Bosutinib capsule

Drug: Bosutinib capsule

Drug: Bosutinib capsule

Bosutinib intact capsules

Active Comparator group

Description:

Bosutinib intact capsules to healthy participants

Treatment:

Drug: Bosutinib capsule

Drug: Bosutinib capsule

Drug: Bosutinib capsule