AZD0284: An Oral RORgt Inverse Agonist
AZD0284
oral RORC2 inverse agonist for psoriasis 100 mg PO BID, Ph. I term. due to preclin. Data from opt. of lit. inverse agonist Journal of Medicinal Chemistry AstraZeneca, Gothenburg, Sweden
Other molecules you may be interested in
BMS-986251
BMS-986251 is an inverse agonist of RORgt, a hot target in inflammation for a significant period. Unfortunately it looks like development hit a wall in this space, and several publications of various company’s RORgt modulators have appeared in the last several months. Chemically, 251 is interesting with 5 stereocenters, none of which look [...]
BI 730357
The Boehringer RORγ antagonist, BI 730357, is an oral once-daily clinical candidate from a new compound class in development for plaque psoriasis. We highlighted two other RORγ modulators last year in February and March. While most clinical RORγ modulators have discontinued development after reaching Ph. II, BI 730357’s Ph. II trial appears [...]
JTE-052 (delgocitinib)
JTE-052 (delgocitinib) is a pan-JAK kinase inhibitor approved as a topical ointment for treatment of atopic dermatitis in Japan. The compound has an interesting azetidine-containing diazaspirocycle core and a relatively high sp3-fraction for a kinase inhibitor.
BioCryst Kallikrein Inhibitor
The Biocryst oral plasma kallikrein inhibitor, berotralstat (BCX7353) , was recently approved as the first non-steroidal treatment for prevention of hereditary angioedema attacks. The molecule is given orally (150 mg QD) despite having two basic amines. Interestingly for a chronically administered drug, the molecule is noted to have QT [...]
SHR168442
The Eternity Bioscience/Shanghai Hengrui RORγ antagonist, SHR168442, is a skin-restricted, topical compound intended to treat psoriasis. As a master regulator of Th17 immune cells which are significantly involved in allergic diseases, both positive and negative oral modulators of RORγt had been hotly pursued, though many have ceased clinical [...]