molecules of the month


oral CNS-penetrant Nav1.7/1.8 blocker

in vivo efficacy in rodent pain models

electrophysiology-based HTS and opt.

Bioorg. Med. Chem.

AbbVie, North Chicago, IL

ABBV-318, oral CNS-penetrant Nav1.7/1.8 blocker - AbbVie, North Chicago, IL
4 mins read

Context. ABBV-318 (AbbVie) is a CNS-penetrating, oral inhibitor of Nav1.7/Nav1.8 being developed for pain treatment. Despite being a highly validated pain target due to its important role in excitable cells, Nav1.7 inhibition has not lived up to its potential, and translation of the promising preclinical observations to human studies has been elusive. A close isoform, Nav1.8, which has mostly encountered similar fates (e.g. XEN-402) in preclinical and clinical studies as Nav1.7, has recently entered the spotlight following a Ph. II readout from Vertex that reported positive data for the Nav1.8 inhibitor VX-548 (structure undisclosed, but related to prodrug VX-150). Similar to Nav1.7, Nav1.8 has been implicated as a key mediator of inflammatory pain, suggesting that a dual Nav1.7/Nav1.8 inhibitor may…

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