Development of Antagonists to ROR-gamma


Orphagen has pioneered the discovery of selective small molecule inhibitors of the orphan nuclear receptor RORγ. RORγ controls the activity of the class of T helper cells known as Th-17 cells. Th-17 cells are involved in a wide range of inflammatory disease.

Orphagen signed an industry partnership with the Pharmaceutical Division of Japan Tobacco for further development of RORγ antagonists in 2008. The partnership was the first of many preclinical-stage partnerships for RORγ antagonists that have swept the pharmaceutical industry. Merck, Pfizer, Amgen, J&J, Sanofi-Aventis and AstraZeneca later entered separate partnerships with early stage companies.

The Pharmaceutical Division of Japan Tobacco is currently undertaking a Phase 2 clinical trial for JTE-451, an RORγ antagonist. Its program is currently the most advanced in the industry. The RORγ program demonstrated Orphagen’s capability to successfully initiate first-in-class discovery.