ArticleMolecular pharmacology2024
State-Dependent Inhibition of Nav1.8 Sodium Channels by VX-150 and VX-548.
Article in Molecular pharmacology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
38 citing papers in PubMed.
- First-in-Human Phase I Trial of HRS-2129, a Selective Nav1.8 Inhibitor: Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics in Healthy Subjects.Drug design, development and therapy · 2026Trial
- A designer saxitoxin-engineered sodium channel pair as a general tool for subtype-selective inhibition.Cell chemical biology · 2026Article
- Chasing the Wrong Door for 30 Years: Is Suzetrigine the Key to Selective Pain Relief?Medicina (Kaunas, Lithuania) · 2026Review
- Review
- Functional characterization of human iPSC-derived sensory neuron processes in microfluidic cultures.Stem cells translational medicine · 2026Article
- Functional role of Nav1.8 channels in action potentials of mouse CGRP-lineage dorsal root ganglion neurons.The Journal of physiology · 2026Article
- Voltage-gated sodium channels in the nervous system: Molecular physiology to therapeutic interventions.Neural regeneration research · 2026Article
- Article
- Discovery and Optimization of Potent and Subtype-Selective Urea-Derived NaACS medicinal chemistry letters · 2026Article
- Novel Ligands for the Orphan Receptor GPR151 Modulate Morphine Action.Genes to cells : devoted to molecular & cellular mechanisms · 2026Article
- The Excelsatoxin A-Receptor TMEM233 Modulates Nav1.8.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026Article
- Extended local anesthesia enabled by flavonoid permeation enhancers.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- A small lipidated peptide targeting NaOsteoarthritis and cartilage open · 2026Article
- Targeting NaInternational journal of molecular sciences · 2026Review
- Suzetrigine, a NaMolecules (Basel, Switzerland) · 2026Review
- Modulation of ion channels as emerging therapeutic targets in the treatment of diabetic neuropathy.EXCLI journal · 2026Review
- Breaking Through Cancer Pain: From Single-Drug Management to Multimodal Analgesia.Pain research & management · 2026Review
- From ion channel biology to clinical practice: suzetrigine as a precision analgesic.Frontiers in medicine · 2026Review
- Toward Brain NaPharmaceuticals (Basel, Switzerland) · 2025Article
- Pharmacological inhibition of NaV1.8 by suzetrigine reveals potent analgesic potential without tolerance development in mice.Molecular brain · 2025Article
Corrections and comments
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Authors and funding
7 authors.
Funding
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
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.