molecules of the month

BAY 1101042 (runcaciguat)

oral once-daily sGC activator

Ph. II for CKD + diabetic neuropathy

from cell-based HTS + opt

J. Med. Chem., Apr. 19, 2021

Bayer AG, Wuppertal, DE

1 min read

The Bayer soluble guanylate cyclase (sGC) activator, BAY 1101042 (runcaciguat), is a once-daily (50 mg), oral clinical candidate in Ph. II for chronic kidney disease and diabetic retinopathy. sGC is an intracellular receptor for nitric oxide (NO), binding NO via a heme-cofactor, which activates a catalytic domain that leads to production of second messenger cGMP. This NO-sGC-cGMP axis is a key pathway regulating the cardiovascular system. Runcaciguat acts by displacing the heme- cofactor, but binding in a way that activates sGC as if NO had bound heme, turning on cGMP production. This conveniently dosed candidate can be useful in evaluating the NO-sGC-cGMP axis in humans in multiple disease contexts.

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