Cenopodlin

Cenopodlin is a small molecule inhibitor of Enhancer of Zeste Homolog 2 (EZH2) being developed by Aurigene Discovery Technologies for the treatment of lymphomas. EZH2 is a histone methyltransferase and the catalytic subunit of the Polycomb Repressive Complex 2 (PRC2), which silences gene expression by trimethylating lysine 27 of histone H3 (H3K27me3). Overexpression or gain-of-function mutations of EZH2 are common in various hematological malignancies, leading to the repression of genes that regulate the cell cycle and differentiation. Cenopodlin is designed to selectively inhibit EZH2 activity, thereby reducing H3K27me3 levels and re-activating tumor suppressor genes to inhibit cancer cell proliferation. It is currently in Phase 1 clinical trials.