HAN Rui, CAI Yi-lin, ZHENG Xiao-tong, LIN Fan-qi, ZHANG Fan. Development of analgesic drugs targeting Nav1.7: advances in clinical trials and discovery of selective inhibitorsJ. Acta Pharmaceutica Sinica, 2024, 59(9): 2417-2428. DOI: 10.16438/j.0513-4870.2024-0259
Citation: HAN Rui, CAI Yi-lin, ZHENG Xiao-tong, LIN Fan-qi, ZHANG Fan. Development of analgesic drugs targeting Nav1.7: advances in clinical trials and discovery of selective inhibitorsJ. Acta Pharmaceutica Sinica, 2024, 59(9): 2417-2428. DOI: 10.16438/j.0513-4870.2024-0259

Development of analgesic drugs targeting Nav1.7: advances in clinical trials and discovery of selective inhibitors

  • The voltage-gated sodium channel subtype Nav1.7 is highly expressed in nociceptive sensory neurons and is a key pathogenic target in several human hereditary pain syndromes. In recent years, a large number of studies have shown that Nav1.7 plays an important role in inflammatory, neuropathic, and nociceptive pain. Therefore, targeting Nav1.7 is a new strategy and hotspot for the development of novel analgesics. This review introduces the structure and function of Nav1.7, its regulatory role in pain, highlights the development progress of small-molecule Nav1.7 inhibitors in clinical trials, and analyzes the preclinical development of highly specific Nav1.7 inhibitors, with a view to providing reference for the development of Nav1.7 analgesic drugs.
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