Resiniferatoxin: Nature's Precision Medicine to Silence TRPV1-Positive Afferents

Int J Mol Sci. 2023 Oct 10;24(20):15042. doi: 10.3390/ijms242015042.

Abstract

Resiniferatoxin (RTX) is an ultrapotent capsaicin analog with a unique spectrum of pharmacological actions. The therapeutic window of RTX is broad, allowing for the full desensitization of pain perception and neurogenic inflammation without causing unacceptable side effects. Intravesical RTX was shown to restore continence in a subset of patients with idiopathic and neurogenic detrusor overactivity. RTX can also ablate sensory neurons as a "molecular scalpel" to achieve permanent analgesia. This targeted (intrathecal or epidural) RTX therapy holds great promise in cancer pain management. Intra-articular RTX is undergoing clinical trials to treat moderate-to-severe knee pain in patients with osteoarthritis. Similar targeted approaches may be useful in the management of post-operative pain or pain associated with severe burn injuries. The current state of this field is reviewed, from preclinical studies through veterinary medicine to clinical trials.

Keywords: TRPV1 receptor; cancer pain; capsaicin; incontinence; osteoarthritic pain; resiniferatoxin.

Publication types

  • Review

MeSH terms

  • Diterpenes* / adverse effects
  • Humans
  • Pain / drug therapy
  • Precision Medicine / adverse effects
  • TRPV Cation Channels / genetics
  • Urinary Bladder, Overactive* / etiology

Substances

  • resiniferatoxin
  • Diterpenes
  • TRPV Cation Channels
  • TRPV1 protein, human

Grants and funding

This research received no external funding.