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
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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