BHV-2100

BHV-2100 is a first-in-class, orally administered, highly selective and potent small molecule antagonist of the transient receptor potential cation channel subfamily M member 3 (TRPM3). It is being developed as a novel, non-sedating, non-opioid treatment for migraine and various pain disorders including neuropathic pain, chemotherapy-induced neuropathy, diabetic neuropathy, and nerve injury. TRPM3 is a calcium-permeable ion channel expressed in sensory neurons of the trigeminal ganglion and dorsal root ganglion that plays a key role in neuroinflammatory pain signal transmission. By antagonizing TRPM3, BHV-2100 inhibits neurogenic inflammation and nociceptor sensitization/activation associated with migraine and pain states. Preclinical studies have shown that BHV-2100 reverses pain without causing sedation or thermoregulatory side effects typical of other TRP antagonists or standard-of-care analgesics. The drug has demonstrated excellent safety/tolerability profiles in early clinical trials[1][2][3][4][5][6][8].