Effect of Valemetostat on the Pharmacokinetics of Midazolam and Digoxin: A Phase 1 Drug-Drug Interaction Study in Patients With Non-Hodgkin Lymphoma.

ABSTRACT: Valemetostat tosylate (valemetostat) is an oral, potent, dual inhibitor of enhancer of zeste homolog (EZH)2/1, under investigation in non-Hodgkin lymphomas (NHLs) and solid tumors. In vitro, it inhibits cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp) when combined with sensitive CYP3A or P-gp substrates. This drug-drug interaction (DDI) sub-study is part of the phase 1 trial of valemetostat monotherapy (DS3201-A-J101; NCT02732275), assessing the effect of valemetostat on the pharmacokinetics (PK) of sensitive CYP3A and P-gp substrates midazolam and digoxin, respectively, in patients with relapsed or refractory NHL, and its safety and efficacy. Patients received two simultaneous single doses of midazolam and digoxin: once alone and once concomitantly with a daily 200 mg valemetostat do

SUBMITTER: Tachibana M 

PROVIDER: S-EPMC12560943 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature