molecules of the month

BAY 1003803

non-steroid glucocorticoid receptor modulator

completed Ph. I as topical agent in psoriasis

from optimization of prior lead

Bioorg. Med. Chem. Lett., Jun. 1, 2020

Bayer AG, Berlin, DE / AstraZeneca

Structure of glucocorticoid receptor agonist BAY 1003803
1 min read

BAY 1003803 is a potent topical agonist of the glucocorticoid receptor (GR) transrepression pathway, with less activity on the GR transactivation pathway mediated by GR dimers, which may lead to undesirable side effects. The fluoroaminoquinoline was the only heterocycle among analogs tested that was Ames-negative. The compound appears to have completed a Ph. I study in 2017, but there don’t appear to be any recent updates.

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