Neurology

Cell culture and mouse studies identified a quinolone sulfonamide-based Nav1.7 antagonist that could help treat pain. Chemical synthesis and testing in HEK cell-based activity assays of quinolone sulfonamide analogs yielded a compound antagonized human and mouse Nav1.7 with IC₅₀ values of 8.5 and 18.6 nM, respectively. In two mouse models of chemical-induced pain, the compound decreased pain-related behaviors compared with vehicle. In a mouse model of irradiation-induced pain, the compound decreased thermal hyperalgesia. Next steps by Amgen Inc. could include testing the compound in additional pain models.

Biogen Inc. has raxatrigine (BIIB074), a state-dependent Nav1.7 inhibitor, in Phase II testing to treat pain...