Novel sodium channel antagonists in the treatment of neuropathic pain

Expert Opin Investig Drugs. 2016;25(2):215-26. doi: 10.1517/13543784.2016.1121992. Epub 2015 Dec 14.

Abstract

Introduction: Effective and safe drugs for the treatment of neuropathic pain are still an unmet clinical need. Neuropathic pain, caused by a lesion or disease that affects the somatosensory system, is a debilitating and hampering condition that has a great economic cost and, above all, a tremendous impact on the quality of life. Sodium channels are one of the major players in generating and propagating action potentials. They represent an appealing target for researchers involved in the development of new and safer drugs useful in the treatment of neuropathic pain. The actual goal for researchers is to target sodium channels selectively to stop the abnormal signaling that characterizes neuropathic pain while leaving normal somatosensory functions intact.

Areas covered: This review covers the most recent publications regarding sodium channel blockers and their development as new treatments for neuropathic pain. The main areas discussed are the natural sources of new blockers, such as venom extracts and the recent efforts from many pharmaceutical companies in the field.

Expert opinion: There have been serious efforts by both the pharmaceutical industry and academia to develop new and safer therapeutic options for neuropathic pain. A number of different strategies have been undertaken; the main efforts directed towards the identification of selective blockers starting from both natural products or screening chemical libraries. At this time, researchers have identified and characterized selective compounds against NaV1.7 or NaV1.8 voltage-gated sodium channels but only time will tell if they reach the market.

Keywords: Neuropathic pain; pain; sodium channel blockers; sodium channel isoforms.

Publication types

  • Review

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Drug Design*
  • Humans
  • Molecular Targeted Therapy
  • Neuralgia / drug therapy*
  • Neuralgia / physiopathology
  • Quality of Life
  • Signal Transduction / drug effects
  • Sodium Channel Blockers / adverse effects
  • Sodium Channel Blockers / pharmacology
  • Sodium Channel Blockers / therapeutic use*
  • Sodium Channels / drug effects
  • Sodium Channels / metabolism

Substances

  • Sodium Channel Blockers
  • Sodium Channels