GNE-616 (GNE616) is a highly potent, metabolically stable, subtype selective inhibitor of Nav1.7 with Ki of 0.79 nM (hNav1.7).
GNE-616 shows robust, concentration dependent reduction in nociceptive events with an EC50 of 740 nM.
GNE-616 is a highly potent inhibitor of Nav1.7 in manual patch clamp electrophysiology assays (Kd=0.38 nM), showing >1000-fold selectivity over Nav1.1, Nav1.3, Nav1.4, and Nav1.5 and modest selectivity over Nav1.2 and Nav1.6 (30-70 fold).
GNE-616 shows a robust PK/PD response in a Nav1.7 dependent mouse model.
