Orphagen Pharmaceuticals, a privately-held pharmaceutical company, announced today that it has been awarded US patent 8,389,739 for modulators of retinoid-related orphan receptor gamma (RORγ). The patent is Orphagen’s first in the RORγ field and describes several small molecule antagonists to RORγ and their effect on Th-17 cell regulation. Orphagen demonstrated that RORγ could, in fact, be regulated by small molecule ligands, establishing the receptor as a valuable new drug target for autoimmune disease.
“We are delighted to have this patent awarded in what has become a highly competitive field,” said Scott Thacher, Orphagen CEO, and lead inventor on the patent. “The patent is recognition of the early technology that established Orphagen as a leader in the identification of small molecule ligands to orphan nuclear receptors. It is clear validation of Orphagen’s business model to de-orphanize nuclear receptors for the development of entirely new therapeutic classes.”
RORγ is a member of the nuclear receptor superfamily of ligand-activated transcription factors, and is considered to be the “master regulator” of Th-17 cells, which were first described in 2005. In 2006, the critical involvement of RORγ was published. The published patent demonstrates that antagonists to RORγ, which could be administered orally, have the potential to specifically suppress Th-17 function for the targeted treatment of conditions like psoriasis and multiple sclerosis. Orphagen’s RORγ antagonists are being developed in partnership with Japan Tobacco.
Orphagen has taken an industry-leading position in the identification and characterization of drugs targeting previously unexplored orphan receptors. Orphagen’s strategy is to validate new targets in cellular and animal models before securing a partner to complete development and commercialization. Orphagen has now identified the first small molecule ligands to three orphan nuclear receptors including RORγ.
About Orphagen: Orphagen discovers drug candidates for potential drug targets for which small molecule ligands–potential drug-like molecules–have yet to be identified. Its goal is to identify, characterize, and position a new class of drug so that pre-clinical and clinical development can be initiated with partners and/or outside sources of funding. These targets come from the nuclear receptor family of drug targets. On a per target basis, the nuclear receptors are one of the most successful target classes known to the pharmaceutical industry. Targets of interest to Orphagen encompass several of the so-called orphan nuclear receptors—potential therapeutic receptors that have yet to be exploited by the pharmaceutical industry.
For more information, contact: Scott Thacher, (858) 481-6191