GDC-0276

GDC-0276 is a novel, potent, selective, and orally bioavailable small molecule inhibitor of the voltage-gated sodium channel NaV1.7. It was developed as a non-opioid analgesic for the treatment of pain, aiming to address limitations of current pain therapies such as inadequate relief and dose-limiting adverse effects. NaV1.7 channels are crucial for pain transduction; genetic evidence supports their role in human pain signaling. GDC-0276 demonstrates high selectivity for NaV1.7 over other sodium channel subtypes and has shown efficacy in preclinical models of inherited erythromelalgia and other pain-related conditions[2][3][5][8]. The drug has undergone phase I clinical trials evaluating its safety, tolerability, and pharmacokinetics in healthy subjects[2]. Developers include Xenon Pharmaceuticals (originator) and Genentech.

Other names

Benzamide N-(1-azetidinylsulfonyl)-5-cyclopropyl-2-fluoro-4-(adamantan-1-ylmethoxy)1494581-70-2