Upcoming topical TRPV1 anti-pruritic compounds

Dermatol Online J. 2020 Sep 15;26(9):13030/qt188477hq.

Abstract

Transient receptor potential vanilloid type 1 (TRPV1) is found on sensory neurons, keratinocytes, sebocytes, and dendritic cells. Activated TRPV1 channels are believed to help propagate the itch sensation. Therefore, there has been great interest in targeting TRPV1 to treat pruritus. Since oral formulations aimed at TRPV1 have led to adverse effects such as hyperthermia, there has been emphasis on developing novel topical agents. Several companies are investigating topical TRPV1 anti-pruritic compounds and the initial data has been very promising. These drugs have the potential to be important treatment options for the management of itch. This paper reviews topical products in current development for pruritus that target TRPV1 channels.

Publication types

  • Review

MeSH terms

  • Acrylamides / therapeutic use
  • Administration, Cutaneous
  • Antipruritics / therapeutic use*
  • Clinical Trials as Topic
  • Heterocyclic Compounds, 4 or More Rings / therapeutic use
  • Humans
  • Pruritus / drug therapy*
  • Pyridines / therapeutic use
  • Receptor, trkA / antagonists & inhibitors
  • Sodium Channel Blockers / therapeutic use
  • TRPV Cation Channels / antagonists & inhibitors*

Substances

  • Acrylamides
  • Antipruritics
  • Heterocyclic Compounds, 4 or More Rings
  • N-(1-(3,5-difluoro-4-methanesulfonylaminophenyl)ethyl)-3-(2-propyl-6-trifluoromethylpyridine-3-yl)acrylamide
  • NTRK1 protein, human
  • Pyridines
  • Sodium Channel Blockers
  • TRPV Cation Channels
  • TRPV1 protein, human
  • pegcantratinib
  • Receptor, trkA