Phase 1
N=18
Bioavailability of Bosutinib Administered as Capsule Contents Mixed With Applesauce or Yogurt Relative to Intact Capsules Under Fed Condition
Healthy Participants
Bottom Line
View on ClinicalTrials.gov: NCT04916769 ↗Enrolled (actual)
18
Serious AEs
0.0%
Results posted
Nov 2024
Primary outcome: Primary: Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib — 3312; 3205; 3161 nanogram•hour per milliliter (ng•hr/mL)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Bosutinib capsule (Drug)
- Age
- Adult · 18+ yrs
- Sex
- All
- Sponsor
- Pfizer
- Primary completion
- Jan 2022
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib |
3312; 3205; 3161 | — |
| PRIMARY Maximum Observed Plasma Concentration (Cmax) for Bosutinib |
126.5; 126.1; 132.0 | — |
| SECONDARY Area Under the Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) for Bosutinib |
3150; 3055; 3009 | — |
| SECONDARY Time to Reach Maximum Observed Plasma Concentration (Tmax) for Bosutinib |
6.00; 6.00; 6.00 | — |
| SECONDARY Apparent Clearance After Oral Dose (CL/F) for Bosutinib |
151.0; 156.0; 158.1 | — |
| SECONDARY Apparent Volume of Distribution After Oral Dose (Vz/F) for Bosutinib |
7903; 8106; 8145 | — |
| SECONDARY Terminal Phase Half-life (t½ ) for Bosutinib |
36.46; 36.30; 36.02 | — |
| SECONDARY Number of Participants With Laboratory Abnormalities |
8; 11; 11 | — |
| SECONDARY Number of Participants With Treatment-emergent Adverse Events (TEAEs), Severe Adverse Events (AEs), and Serious Adverse Events (SAEs) |
11; 14; 15; 0; 0; 0 | — |
Summary
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.
Eligibility Criteria
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:
- estimated glomerular filtration rate (eGFR) (Chronic Kidney Disease Epidemiology Collaboration [CKD-EPI]) 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.
Data sourced from ClinicalTrials.gov (NCT04916769). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.