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ACT-1117-2520 (also known as IDOR-1117-2520C) is a potent, selective, and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor gamma t (RORγt), developed by Idorsia Pharmaceuticals. RORγt is a master transcription factor essential for the differentiation of Th17 cells and the subsequent production of pro-inflammatory cytokines, including IL-17A, IL-17F, and IL-22. These cytokines are central to the pathophysiology of various autoimmune and inflammatory conditions, particularly psoriasis and psoriatic arthritis. By binding to the ligand-binding domain of RORγt, ACT-1117-2520 suppresses the transcriptional activity of the receptor, thereby reducing the Th17-mediated inflammatory cascade. The compound has been evaluated in Phase 2 clinical trials for moderate to severe chronic plaque psoriasis, demonstrating its potential as an oral therapeutic alternative to injectable biologics.
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