Phase 1 study of GSK3368715, a type I PRMT inhibitor, in patients with advanced solid tumors.

ABSTRACT:

Background

GSK3368715, a first-in-class, reversible inhibitor of type I protein methyltransferases (PRMTs) demonstrated anticancer activity in preclinical studies. This Phase 1 study (NCT03666988) evaluated safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy of GSK3368715 in adults with advanced-stage solid tumors.

Methods

In part 1, escalating doses of oral once-daily GSK3368715 (50, 100, and 200 mg) were evaluated. Enrollment was paused at 200 mg following a higher-than-expected incidence of thromboembolic events (TEEs) among the first 19 participants, resuming under a protocol amendment starting at 100 mg. Part 2 (to evaluate preliminary efficacy) was not initiated.

Results

Dose-limiting toxicities were reported in 3/12 (25%) patients at 200 mg. Ni

SUBMITTER: El-Khoueiry AB 

PROVIDER: S-EPMC10338470 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature