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

AB El-Khoueiry; J Clarke; T Neff; T Crossman; N Ratia; C Rathi; P Noto; A Tarkar; I Garrido-Laguna; E Calvo; J Rodón; B Tran; PJ O’Dwyer; A Cuker; AR Abdul Razak

Journal article

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

AB El-Khoueiry, J Clarke, T Neff, T Crossman, N Ratia, C Rathi, P Noto, A Tarkar, I Garrido-Laguna, E Calvo, J Rodón, B Tran, PJ O’Dwyer, A Cuker, AR Abdul Razak

British Journal of Cancer | Published : 2023

DOI: 10.1038/s41416-023-02276-0

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. Res..

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University of Melbourne Researchers

Ben Tran Author

Grants

Funding Acknowledgements

Authors who are or were employees of GSK contributed to the design of the study, analysis of the data, and in the decision to publish for this study (NCT03666988 available from www.clinicaltrials.gov) was provided by GSK. Open access funding provided by SCELC, Statewide California Electronic Library Consortium.