Inhibiting Nav1.8 for pain: Lessons from patients and from neurons
Abstract
analgesics, with peripheral Na + channels that mediate pain signaling within the PNS emerging as major targets. Identification of Nav1.8 as a peripherally restricted Na + channel ( 1 ) and demonstration of its powerful role as a driver of pain signaling ( 2 , 3 ) have been followed by efforts to develop subtype - specific Nav1.8 inhibitors. One of these Nav1.8 inhibitors, suzetrigine, is ~ 31,000 - fold selective over other Na + channels ( 4 ). Recent clinical trials of this Nav1.8 blocker in acute postoperative pain have provided proof - of - concept that inhibition of Nav1.8 can reduce pain in humans ( 5 , 6 ). In these trials, pain was reduced by ~ 1 to 2 points (within an 11 - point rating scale); responsiveness differed (30 to 70%) among subjects ( 5 ). What might we learn from the less - than - full pain relief seen with treatment with this highly subtype - specific Nav1.8 inhibitor?
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