Resiniferatoxin: Mechanism in Treating Osteoarthritis Pain and Slowing Osteoarthritis Progression, Safety, and Efficacy

Resiniferatoxin is a diterpene found in E. resinifera and E. poissonii, and is a more potent functional analog of capsaicin. Resiniferatoxin provides pain relief by binding as an agonist to transient vanilloid receptor 1 (TRPV1), a nociceptive ion channel. Resiniferatoxin targets the TRPV1 channel and activates it, allowing calcium cations to flow in and desensitize the TRPV1 receptors, producing an analgesic effect. Resiniferatoxin was recently designated as a Breakthrough Therapy by the FDA for the treatment of the pain caused by knee osteoarthritis, a common degenerative joint disease caused by aging, joint injury, and obesity. Studies suggest that osteoarthritis is linked with chronic inflammation through a cycle of injury, inflammation, and repair. Multiple studies involving TRPV1 agonists have shown anti-inflammatory properties, presenting TRPV1 agonists as a potential inhibitor for the progression of osteoarthritis. This review highlights the mechanism of resiniferatoxin in treating pain caused by knee osteoarthritis, its potential in treating inflammation in osteoarthritis, its efficacy, and its safety.