GDC-0310

GDC-0310 is a selective, orally bioavailable small molecule inhibitor of the voltage-gated sodium channel Nav1.7 (encoded by SCN9A), developed as a non-opioid analgesic for the treatment of pain. It is an acyl-sulfonamide compound with high potency (IC50 = 0.6 nM for human Nav1.7) and significant selectivity over other sodium channel subtypes, though its selectivity over Nav1.4 is modest compared to other isoforms[1][5][8]. The drug was designed to block pain signaling by inhibiting Nav1.7, a target genetically validated in humans with congenital insensitivity to pain[7][8]. GDC-0310 completed Phase I clinical trials but was discontinued from further development due to undisclosed reasons[2][3][8]. The compound was co-developed by Genentech and Xenon Pharmaceuticals.