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

VernacularTitle:靶向Nav1.7的镇痛药物开发: 临床试验进展与选择性抑制剂发现
Author: Rui HAN ; Yi-lin CAI ; Xiao-tong ZHENG ; Fan-qi LIN ; Fan ZHANG
Publication Type:Research Article
Keywords: Nav1.7; pain; analgesic drug; clinical trial; selective inhibitor
From: Acta Pharmaceutica Sinica 2024;59(9):2417-2428
CountryChina
Language:Chinese
Abstract: 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.