Zucapsaicin for the treatment of neuropathic pain

Expert Opin Investig Drugs. 2014 Oct;23(10):1433-40. doi: 10.1517/13543784.2014.956079. Epub 2014 Aug 29.


Introduction: Neuropathic pain (NP) is a chronic disease that stems from a primary lesion or dysfunction of the central or peripheral nervous system. Zucapsaicin is a synthetic cis isomer of natural capsaicin that has shown therapeutic efficacy in pain accompanying osteoarthritis of the knee. It is also currently under investigation for the relief of severe pain in adults suffering from NP.

Areas covered: The authors provide an overview of the pharmacological properties of zucapsaicin based on available data from both preclinical and clinical trials. They also discuss its mechanism of action.

Expert opinion: The mechanism of action and clinical indications of zucapsaicin are similar to that of its naturally occurring isomer, capsaicin. However, in contrast to capsaicin, zucapsaicin is better tolerated. In the future, zucapsaicin could become a valuable drug for treating pain relief. Indeed, it is possible, in addition to providing NP relief, that it may have a use in treating osteoarthritic pain, headaches and pain that accompany intestinal diseases.

Keywords: TRPV1 agonist; neuropathic pain; topical analgesics; zucapsaicin.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Adult
  • Analgesics / adverse effects
  • Analgesics / pharmacology
  • Analgesics / therapeutic use*
  • Animals
  • Capsaicin / adverse effects
  • Capsaicin / analogs & derivatives*
  • Capsaicin / pharmacology
  • Capsaicin / therapeutic use
  • Headache / drug therapy
  • Humans
  • Neuralgia / drug therapy*
  • Neuralgia / physiopathology
  • Osteoarthritis, Knee / drug therapy
  • Pain / drug therapy
  • Pain / etiology
  • Severity of Illness Index


  • Analgesics
  • zucapsaicin
  • Capsaicin