molecules of the month

Context. EZM0414 (Epizyme, Inc.) is an oral SETD2 inhibitor being developed for hematological malignancies. Although several genetic studies have proposed that the histone methyltransferase SETD2 is a tumor suppressor in solid cancers, inhibition of the enzyme may be desirable in some hematological malignancies such as leukemia and lymphoma. In particular, certain mutations in multiple myeloma (MM) and diffuse large B-cell lymphoma (DLBCL) that result in dysregulation of histone H3 lysine 36 (H3K36) methylation are thought to be key to tumorigenesis in these malignancies. The FDA recently granted Fast Track Status to EZM0414, which is currently being evaluated in a Ph. I study. Epizyme, and with it EZM0414, was recently acquired by Ipsen as part of a $247 million deal that…