arn-6039

ARN-6039 is a potent, orally available small molecule inverse agonist of RORγt (RAR-related orphan receptor gamma t), a nuclear hormone receptor and key transcription factor that regulates the differentiation and function of Th17 cells. Th17 cells are implicated in the pathogenesis of several autoimmune diseases through their production of pro-inflammatory cytokines such as IL-17 and IL-17A. By inhibiting RORγt, ARN-6039 suppresses Th17 cell differentiation and reduces IL-17-mediated inflammation. The drug was discovered by Arrien Pharmaceuticals using their proprietary fragment-based FIELDS technology platform. Preclinical studies demonstrated efficacy in models of autoimmune demyelinating disease (such as experimental autoimmune encephalomyelitis) with good CNS penetration and safety profile. Clinical development has focused on multiple sclerosis (MS), with additional interest in psoriasis and other immune-mediated disorders[4][5][6][7][8][9].

Other names

ARN 6039ARN6039ARN-6039