Nav1.8 in the spotlight: A non-opioid pain solution emerges

A recent study by Vertex Pharmaceuticals, published in Pain and Therapy, showcases the potential of suzetrigine, a Nav1.8-selective inhibitor, as a promising non-opioid analgesic. This work is a significant milestone in ion channel research, particularly for pain management.

Using Qube automated patch clamp, suzetrigine was shown to have remarkable selectivity for Na_v1.8 channels, critical players in pain signaling, with an IC50 of 0.68 nM, making it 30,000 times less potent against other Na_v1.x channels. Electrophysiological studies in human sensory neurons confirmed suzetrigine’s ability to inhibit action potential firing at nanomolar concentrations. Clinical trials, including a post-surgical pain model, highlighted its effectiveness in managing acute pain, with a favorable safety and non-addictive profile.

The study underscores Na_v1.8’s potential as a target for addressing acute pain without the risks of addiction associated with opioids. This research represents a crucial step forward for non-opioid therapeutics, offering hope for safer and more effective pain management solutions.

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