Phase 1
Completed N=32
Evaluation of the Relative Bioavailability of Bosutinib Capsules Under Fed Condition and Estimation of Food Effect on Orally Administered Bosutinib Capsule
Healthy Participants
Source: ClinicalTrials.gov NCT05032690 ↗
Enrolled (actual)
32
Serious AEs
0.0%
Results posted
Sep 2024
Primary outcomePrimary: Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib — 591.3; 591.7; 479.4 nanogram*hour per milliliter (ng*hr/mL)
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Concentration-time Curve From Time 0 to Infinity (AUCinf) for Bosutinib |
591.3; 591.7; 479.4 | — |
| PRIMARY Maximum Observed Plasma Concentration (Cmax) for Bosutinib |
17.80; 16.68; 10.75 | — |
| SECONDARY Area Under the Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) for Bosutinib |
455.6; 446.4; 301.6 | — |
| SECONDARY Time for Cmax (Tmax) of Bosutinib |
6.00; 6.00; 6.00 | — |
| SECONDARY Apparent Clearance After Oral Dose (CL/F) of Bosutinib |
169.3; 169.0; 208.5 | — |
| SECONDARY Apparent Volume of Distribution After Oral Dose (Vz/F) of Bosutinib |
11130; 10650; 12870 | — |
| SECONDARY Terminal Elimination Half-Life (t1/2) of Bosutinib |
47.22; 46.01; 43.28 | — |
| SECONDARY Number of Participants With Laboratory Abnormalities (Without Regard to Baseline Abnormality) |
7; 8; 3; 1; 0; 0 | — |
| SECONDARY Number of Participants With Treatment-Emergent Adverse Events (TEAEs) |
13; 20; 5; 0; 0; 0 | — |
Eligibility Criteria
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]) 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 (NCT05032690). 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. Informational only — not medical advice.