Iadarola Michael J, Sapio Matthew R, Nahama Alexis, Mannes Andrew J
Department of Perioperative Medicine, Clinical Center, National Institutes of Health, Bethesda, MD, USA.
Vivasor Inc., San Diego, CA, USA.
Pain Manag. 2025 Aug 8:1-12. doi: 10.1080/17581869.2025.2535271.
Clinical investigations of resiniferatoxin (RTX) analgesia are currently ongoing for several human pain indications. RTX is an agonist of the TRPV1 receptor cation ion channel which is activated by capsaicin, heat, and inflammatory conditions. RTX injection at peripheral sites of pain generation will produce a chemo-inactivation of local nerve terminals and axons and block the transmission of nociceptive signals to spinal cord. Clinical human studies with RTX to treat osteoarthritis (OA) pain were preceded by extensive animal and cell system testing which revealed mechanisms of action, range of potentially treatable pain problems, and the safety and efficacy of this interventional analgesic agent. The present review concentrates on RTX, but also examines intraarticular (IA) capsaicin, a lower potency TRPV1 agonist, for the same indication. We review studies of RTX in human patients and canine veterinary subjects with OA pain. To date, results of several phase I clinical trials have only been reported in abstract form and these studies, despite their preliminary nature, will be examined herein. The present assessments indicate that RTX has strong therapeutic promise to be an innovative approach to medical management of pain relief in osteoarthritis and may be permissive to beneficial tissue remodeling.
目前正在对树脂毒素（RTX）镇痛进行多项针对人类疼痛适应症的临床研究。RTX是TRPV1受体阳离子离子通道的激动剂，该通道可被辣椒素、热和炎症条件激活。在疼痛产生的外周部位注射RTX将导致局部神经末梢和轴突的化学失活，并阻断伤害性信号向脊髓的传递。在对RTX治疗骨关节炎（OA）疼痛进行临床人体研究之前，进行了广泛的动物和细胞系统测试，揭示了其作用机制、潜在可治疗疼痛问题的范围以及这种介入性镇痛剂的安全性和有效性。本综述主要关注RTX，但也研究了关节内（IA）辣椒素，一种效力较低的TRPV1激动剂，用于相同适应症。我们回顾了RTX在患有OA疼痛的人类患者和犬类兽医受试者中的研究。迄今为止，几项I期临床试验的结果仅以摘要形式报道，尽管这些研究具有初步性质，但本文仍将对其进行研究。目前的评估表明，RTX作为一种创新方法，在骨关节炎疼痛缓解的医学管理方面具有强大的治疗前景，并且可能有利于有益的组织重塑。
