BP, use-dependent sodium channel blocker
Ph. II oral efficacy in trigeminal neuralgia
from cell-based HTS and ligand-based opt.
ACS Med. Chem. Lett., Jul. 16, 2020
biogen / Convergence / GSK, MA / UK
Vixotrigine (BIIB074) is a voltage-gated sodium channel blocker that preferentially binds to the inactivated state of the sodium channels, conferring selectivity for channels involved in pain-associated high frequency nerve signalling over normal low frequency nerve signalling (use-/state-dependence). The use-dependent activity is believed to confer a better safety window over previous generations of sodium channel inhibitors. Two Ph. III clinical trials appear to be planned for trigeminal neuralgia with estimated start dates in mid-2021.