VX-548 (Suzetrigine) is a potent, highly selective and orally bioavailable inhibitor of NaV1.8 voltage-gated sodium channel with IC50 of 0.7 nM. VX-548 (Suzetrigine) displays 31,000-fold selectivity over all other NaV subtypes (i.e., NaV1.1 to NaV1.7, and NaV1.9) in recombinant cells. VX-548 (Suzetrigine) shows subnanomolar potency in primary neurons isolated from human dorsal-root ganglia. In two phase 2 clinical trials of postoperative pain, as compared with placebo, the highest dose, but not lower doses, of VX-548 reduced pain over a 48-hour period.
