ezm0414

EZM0414 is an orally bioavailable, selective small molecule inhibitor of the histone methyltransferase SETD2 (SET domain containing 2, histone lysine methyltransferase). It was developed as a first-in-class agent with potential antineoplastic activity. By binding to and inhibiting the activity of SETD2, which is responsible for trimethylation of lysine 36 on histone H3 (H3K36me3), EZM0414 disrupts epigenetic regulation involved in cancer cell proliferation and survival. The drug was primarily investigated for use in relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma (DLBCL), including t(4;14) and non t(4;14) subtypes. It received orphan drug status for multiple myeloma and fast track designation from the FDA for DLBCL. Development has been discontinued as of late 2024[1][2][3][5][7].

Other names

SETD2 inhibitor EZM0414SETD-2 inhibitor EZM0414SETD 2 inhibitor EZM0414SETD2-IN-1 TFASETD-2-IN-1 TFASETD 2-IN-1 TFA