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resiniferatoxin
- Development stage
- Phase 3
- Lead developer
- Grünenthal
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intrathecal, Intraarticular
01
Overview
Resiniferatoxin is a naturally occurring, ultrapotent capsaicin analog derived from the cactus-like plant Euphorbia resinifera. It acts as a highly potent agonist of the transient receptor potential vanilloid 1 (TRPV1) receptor, which is expressed in a subpopulation of primary afferent sensory neurons involved in nociception and pain transmission. By activating TRPV1, resiniferatoxin causes prolonged channel opening and calcium influx, leading to selective ablation or desensitization of TRPV1-expressing pain fibers. This results in long-lasting analgesia by interrupting chronic pain signaling while sparing other sensory modalities such as mechanosensation and proprioception. Resiniferatoxin has been investigated for use in severe cancer pain (via intrathecal administration), osteoarthritis-related knee pain (via intra-articular injection), neurogenic detrusor overactivity, and other chronic pain conditions. Its mechanism allows for targeted "molecular scalpel" ablation of nociceptive neurons with minimal systemic side effects[1][3][4][5][6][8].
- Brand names
- Lopain
- Other names
- resiniferatoxin
02
Targets
TRPV1 (Transient receptor potential cation channel subfamily V member 1)
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