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EPZ004777

Development stage: Preclinical
Lead developer: Ipsen
Modality: Small Molecules
Administration: Subcutaneous Infusion

Overview

EPZ004777 is a potent and selective inhibitor of DOT1L, a protein methyltransferase responsible for the methylation of lysine 79 on histone H3 (H3K79). It competes with the enzyme's co-factor, S-adenosylmethionine (SAM), and disrupts the catalytic pocket. EPZ004777 effectively inhibits cellular H3K79 methylation, blocking the expression of leukemogenic genes such as *HOXA9* and *MEIS1* in MLL-rearranged leukemia cells. It induces apoptosis in these cells but has little effect on non-MLL-translocated cells. Despite its poor pharmacokinetic properties, EPZ004777 shows promise in mouse models of leukemia.

Targets

TPBG (Trophoblast glycoprotein)PRMT5 (Protein arginine N-methyltransferase 5)DOT1LSNX19 (Sorting nexin-19)

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