Bioavailability, Metabolism, and Excretion of [¹⁴C]-Tazemetostat in Patients With B-Cell Lymphomas or Advanced Solid Tumors.

ABSTRACT: This open-label, multicenter study (NCT03010982) evaluated the absolute bioavailability, characterized the disposition and metabolism, and investigated the metabolic profile of tazemetostat, a US Food and Drug Administration-approved inhibitor of enhancer of zeste homolog 2, following intravenous and oral [¹⁴C]-labeled and unlabeled tazemetostat in patients with B-cell lymphomas or advanced solid tumors. Patients received oral tazemetostat 800 mg twice daily for 14 days. On Day 15, patients received tazemetostat 800-mg tablets in a fasted state followed by an intravenous microdose of 12 µg [¹⁴C]-tazemetostat. On Day 16, patients received a [¹⁴C]-tazemetostat 800-mg solution with a meal, then continued tazemetostat 800 mg twice daily. Blood, plasma, urine, a

SUBMITTER: Chen Y 

PROVIDER: S-EPMC11905873 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature