A Phase 1, Open-label, Single-dose, Randomized Crossover Study to Evaluate the Relative Bioavailability of Two Different Capsule Formulations of Sitravatinib in Healthy Subjects
Overview
- Phase
- Phase 1
- Intervention
- Sitravatinib
- Conditions
- Tumor
- Sponsor
- BeiGene
- Enrollment
- 26
- Locations
- 1
- Primary Endpoint
- Apparent Total Plasma Clearance (CL/F) of Sitravatinib
- Status
- Completed
- Last Updated
- last year
Overview
Brief Summary
The primary objective of the study was to investigate the relative bioavailability and pharmacokinetics (PK) of sitravatinib free base and malate salt capsule formulations following oral administration in healthy adults.
Investigators
Eligibility Criteria
Inclusion Criteria
- •Body mass index between 18.0 and 32.0 kg/m2, inclusive.
- •In good health, determined by no clinically significant findings from medical history, physical examination, 12-lead ECG, vital sign measurements, and clinical laboratory evaluations at Screening and/or Check-in as assessed by the Investigator (or designee).
- •Able to swallow multiple capsules.
Exclusion Criteria
- •History of stomach or intestinal surgery or resection
- •Have previously completed or withdrawn from this study or any other study investigating sitravatinib and have previously received the investigational product.
- •Participants who, in the opinion of the Investigator (or designee), should not participate in this study.
- •NOTE: Other protocol defined Inclusion/Exclusion criteria may apply.
Arms & Interventions
Dosing Sequence 1: Sitravatinib Free Base then Malate Salt
Sitravatinib free base capsule 120 mg on Day 1 in Period 1 then sitravatinib malate salt capsule 100 mg on Day 1 in Period 2, with a minimum washout period between dose administrations of 14 days
Intervention: Sitravatinib
Dosing Sequence 2: Sitravatinib Malate Salt then Free Base
Sitravatinib malate salt capsule 100 mg on Day 1 in Period 1 then sitravatinib free base capsule 120 mg on Day 1 in Period 2, with a minimum washout period between dose administrations of 14 days
Intervention: Sitravatinib
Outcomes
Primary Outcomes
Apparent Total Plasma Clearance (CL/F) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Time of the Maximum Observed Plasma Concentration (Tmax) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Maximum Observed Plasma Concentration (Cmax) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Area Under the Concentration-time Curve From Time Zero to Time of the Last Quantifiable Concentration (AUC0-t) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Area Under the Concentration-time Curve (AUC) From Time Zero to Infinity (AUC0-∞) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Apparent Terminal Elimination Half-life (T1/2) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Apparent Volume of Distribution (Vz/F) of Sitravatinib
Time Frame: Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Secondary Outcomes
- Number of Participants With Adverse Events(Up to Week 8)