molecules of the month


oral NLRP3 inhibitor

predicted human dose of 500 mg QD

LLE opt. and tox. mitig. from prev. clin. Cand.

J. Med. Chem.

Genentech, South San Francisco, CA

GDC-2394 chemical structure oral NLRP3 inhibitor - Genentech, South San Francisco, CA
5 mins read

Context. GDC-2394 (Genentech) is an oral NLRP3 inflammasome inhibitor. The NLRP3 inflammasome is the best studied and most characterized inflammasome, with the protein playing a key role in the detection of inflammatory danger signals which are a hallmark of many inflammatory diseases. Hyperactivation of the NLRP3 has been implicated in the pathogenesis of several diseases of high unmet need, such as autoimmune, chronic inflammatory, and metabolic diseases, making the protein an actively pursued drug target. Despite its appeal, development of agents targeting NLRP3 over the years has been challenged by, among other factors, the scarcity of detailed structural data. The first NLRP3 inhibitor to enter the clinic, Pfizer’s CP-456773 (MCC950, CRID3), was not realized to be an NLRP3 inhibitor at…

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