KRP-KC121E

KRP-KC121E is a small molecule antagonist of the Transient Receptor Potential Vanilloid 1 (TRPV1) channel, developed through a collaboration between Kyorin Pharmaceutical and Senju Pharmaceutical. It was primarily investigated as an ophthalmic instillation for the treatment of Meibomian gland dysfunction (MGD), a condition characterized by terminal duct obstruction and qualitative or quantitative changes in glandular secretion. TRPV1 is a non-selective cation channel that plays a key role in the transmission of pain and the mediation of neurogenic inflammation on the ocular surface. By blocking TRPV1, KRP-KC121E was intended to alleviate the symptoms of MGD. However, a multicenter, randomized Phase 2 trial in Japan failed to demonstrate a statistically significant improvement in the primary endpoint compared to placebo, leading to the cessation of its development for this indication.