Na(v)1.7 inhibitors for the treatment of chronic pain

The voltage gated sodium channel Na(v)1.7 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(v)1.7 inhibitors for the treatment of chronic pain. This digest will introduce the structure and function of Na(v)1.7 and highlight the wealth of recent developments on a diverse array of Na(v)1.7 inhibitors, including optimization of their potency, selectivity, and PK/PD relationships.