Nav1.7 inhibitors for the treatment of chronic pain

The voltage gated sodium channel Na_v1.7 plays an essential role in the transmission of pain signals. Strong human genetic validation has motivated extensive efforts to discover potent, selective, and efficacious Na_v1.7 inhibitors for the treatment of chronic pain. This digest will introduce the structure and function of Na_v1.7 and highlight the wealth of recent developments on a diverse array of Na_v1.7 inhibitors, including optimization of their potency, selectivity, and PK/PD relationships.