State-Dependent Inhibition of Nav1. 8 Sodium Channels by VX-150 and VX-548
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P Vaelli, A Fujita, S Jo, HXB Zhang, T Osorno…
Molecular …, 2024
Elsevier
ABSTRACT Nav1. 8 sodium channels (Nav1. 8) are an attractive therapeutic target for pain because they are prominent in primary pain-sensing neurons with little expression in most other kinds of neurons. Recently, two Nav1. 8-targeted compounds, VX-150 and VX-548, have shown efficacy in clinical trials for reducing pain. We examined the characteristics of Nav1. 8 inhibition by these compounds. The active metabolite form of VX-150 (VX-150m) inhibited human Nav1. 8 channels with an IC 50 of 15 nM. VX-548 (suzetrigine) was even …
