GRC-15300

GRC-15300 is an orally administered small-molecule antagonist of the transient receptor potential vanilloid 3 (TRPV3) ion channel, originally discovered by Glenmark Pharmaceuticals and later out-licensed to Sanofi for development in pain indications.[3][7][11] By selectively inhibiting TRPV3, a heat- and mechanically sensitive cation channel expressed in sensory neurons and keratinocytes that contributes to nociceptive signaling, GRC-15300 was intended as a first-in-class, non-opioid therapy for chronic pain conditions including osteoarthritic and peripheral neuropathic pain.[3][4][5][7] The compound advanced into phase I and subsequently phase II clinical trials for neuropathic pain, but the clinical program was discontinued by 2013 and the Sanofi–Glenmark collaboration was terminated in 2014, with no further development reported and no regulatory approvals obtained.[4][5][7][9][12]