ARN-4079 is a novel, highly selective, irreversible, orally available Janus Kinase 3 (JAK3) inhibitor we have developed, and it targets unique Cys909 residue at the gatekeeper position. ARN-4079 selectively inhibited JAK3 over other JAKs and Cys909 kinome members. A cellular selectivity study demonstrated that ARN-4079 preferentially inhibited JAK3 over JAK1 in JAK/STAT signaling.
ARN-4079 covalently bind to the Cys909 residue in JAK3 was clearly validated and the supportive favorable target profiles, the pharmacokinetic properties and its low toxicity, ARN-4079 exhibit improved efficacy than clinically approved pan-JAK or dual JAK1/JAK3 inhibitors. In our CIA and oxazolone-induced Atopic Dermatitis (AD) mice efficacy studies without any significant adverse effects, ARN-4079 exhibited promising efficacy, safety in RA and AD mice over clinically approved agents.
ARN-4079 is a potent, selective, and durable inhibitor of JAK3 and has the potential for the treatment of inflammatory disorders and autoimmune diseases such; rheumatoid arthritis, atopic dermatitis, alopecia areata, vitiligo and other skin diseases.
ARN-4079 is an IND ready agent and at this stage of development, company is potential seeking an opportunity to partner in order to complete IND enabling studies and to take in to clinical Phase 1 trials.