Preclinical and Clinical Aspects of using Tazemetostate in Human Cancers

Abstract

Epigenetic drugs are novel drug categories with promising effects in different cancers. Tazemetostate is among the drugs that were recently used in clinical settings, especially in the treatment of specific tumors and lymphomas. There are a growing number of ongoing clinical trials evaluating the safety and efficacy of tazemetostate in different cancers. The present review addressed the available preclinical studies evaluating the combination of tazemetostate and other chemotherapy agents in treating different cancers and summarized the limited clinical evidence available regarding the efficacy of this novel Enhancer of Zeste Homolog 2 (EZH2) inhibitor in cancer. Based on the available clinical studies, tazemetostate could be considered a safe epigenetic agent with limited adverse events for treating specific types of lymphomas and solid tumors. However, the superiority of using tazemetostate over other chemotherapy agents in patients with cancer as well as using the drug for other clinical conditions, including non-alcoholic steatohepatitis, needs further investigation. Moreover, the effect of tazemetostate on human germline cells is clearly evaluated as some animal studies demonstrated that the drug can affect germline epigenome suggesting further studies on this issue.

Keywords: Tazemetostate; cancer; chemotherapy; epigenetics; pharmacology; solid tumor.