Relative Bioavailability of Two Different Capsule Formulations of Sitravatinib in Healthy Adults

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

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.

Study Overview

• Status: Completed
• Conditions: Tumor
• Intervention / Treatment: Drug: Sitravatinib; Drug: Sitravatinib

• Study Type: Interventional
• Enrollment (Actual): 26
• Phase: Phase 1

Contacts and Locations

Study Locations

• Australia
  • Western Australia
    • Nedlands, Western Australia, Australia, 6009
      • Linear Clinical Research

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 14 years to 51 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Key Inclusion Criteria:

1. Body mass index between 18.0 and 32.0 kg/m2, inclusive.
2. 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).
3. Able to swallow multiple capsules.

Key Exclusion Criteria:

1. History of stomach or intestinal surgery or resection
2. Have previously completed or withdrawn from this study or any other study investigating sitravatinib and have previously received the investigational product.
3. 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.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: 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	Drug: Sitravatinib; Administered orally as a free base capsule; Drug: Sitravatinib; Administered orally as a malate salt capsule
Experimental: 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	Drug: Sitravatinib; Administered orally as a free base capsule; Drug: Sitravatinib; Administered orally as a malate salt capsule

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area Under the Concentration-time Curve (AUC) From Time Zero to Infinity (AUC0-∞) of Sitravatinib	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	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	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	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	Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period
Apparent Total Plasma Clearance (CL/F) of Sitravatinib	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	Predose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 and 168 hours postdose in each study period

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Number of Participants With Adverse Events	Adverse events (AEs) and serious adverse events are defined as an AE that starts during or after the first dose, or starts prior to the first dose and increases in severity after the first dose, including vital signs, physical examination, electrocardiogram, and laboratory parameters	Up to Week 8

Collaborators and Investigators

• Sponsor: BeiGene
• Investigators: Principal Investigator: Study Director, BeiGene

Study record dates

Study Major Dates

• Study Start (Actual): July 23, 2020
• Primary Completion (Actual): November 9, 2020
• Study Completion (Actual): November 9, 2020

Study Registration Dates

• First Submitted: July 14, 2020
• First Submitted That Met QC Criteria: July 14, 2020
• First Posted (Actual): July 15, 2020

Study Record Updates

• Last Update Posted (Actual): October 26, 2024
• Last Update Submitted That Met QC Criteria: October 23, 2024
• Last Verified: October 1, 2024

More Information

Terms related to this study

• Other Study ID Numbers: BGB-Sitravatinib-101

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: YES

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: Yes