molecules of the month


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

1 min read

The AstraZeneca oral RORgt inverse agonist, AZD0284, is an inverse agonist of the nuclear receptor RORC2 (RORγt). Reviewer Chris Gampe says, “targeting the activation and function of Th17 cells has been successful for the treatment of autoimmune disease (cf. IL-17, IL-17R, IL-23 Abs). RORC2 is the transcription factor that controls Th17 function and is a target of high interest in immunology and immuno-oncology, with at least 12 compounds in clinical development worldwide, and the first signs of clinical efficacy being reported for a compound called VTP-43742.” AZD0284 was well-tolerated in a Ph. I study with biomarker changes observed at low doses (4-238 mg). It will be interesting to see if the molecule is advanced further.

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