molecules of the month

“Compound 72”

oral PRMT5 inh. for treating cancers

projected human dose of 15 mg QD w/ 6 HBD

SBDD from SAM cofactor

J. Med. Chem., Mar. 23, 2021

Merck & Co, Boston, MA

Structure of compound 72
1 min read

The Merck protein arginine methyltransferase 5 (PRMT5) inhibitor (“compound 72”) is a SAM cofactor-mimetic with a novel 5,5-fused carbon-based bicyclic scaffold. PRMT5 is an actively pursued epigenetic target for cancer with a flurry of research programs being published recently and several trials being initiated. Remarkably, compound 72 has an excellent oral PK profile in higher species with a low predicted human dose of 15 mg QD, despite having 6 hydrogen bond donors and 6 rings.

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