Pharmacokinetics and Safety of Ripretinib in Participants with Hepatic Impairment: A Phase 1 Study.

ABSTRACT:

Introduction

Ripretinib, an oral switch-control inhibitor of KIT tyrosine kinase and platelet-derived growth factor receptor alpha kinase, is approved for adults with advanced gastrointestinal stromal tumor who received prior treatment with three or more kinase inhibitors, including imatinib. Ripretinib is metabolized into the equally active major metabolite DP-5439, a prominent component of total drug exposure in humans after oral administration. Ripretinib and DP-5439 undergo hepatic metabolism mainly via cytochrome P450 3A4. Therefore, exposure to ripretinib and/or DP-5439 may be affected in patients with hepatic impairment.

Methods

This is a phase 1, open-label study evaluating the pharmacokinetics and safety of ripretinib and DP-5439 in participants with varying degrees

SUBMITTER: Papinska A 

PROVIDER: S-EPMC12394274 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature