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

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 sho...

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Main Author: Arpad Szallasi
Format: Article
Language:English
Published: MDPI AG 2023-10-01
Series:International Journal of Molecular Sciences
Subjects:
Online Access:https://www.mdpi.com/1422-0067/24/20/15042
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author Arpad Szallasi
author_facet Arpad Szallasi
author_sort Arpad Szallasi
collection DOAJ
description 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.
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spelling doaj.art-894747bb711044328fc68b9f45e9cfec2023-11-19T16:40:45ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-10-0124201504210.3390/ijms242015042Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive AfferentsArpad Szallasi0Department of Pathology and Experimental Cancer Research, Semmelweis University, 1083 Budapest, HungaryResiniferatoxin (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.https://www.mdpi.com/1422-0067/24/20/15042resiniferatoxincapsaicinTRPV1 receptorcancer painosteoarthritic painincontinence
spellingShingle Arpad Szallasi
Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive Afferents
International Journal of Molecular Sciences
resiniferatoxin
capsaicin
TRPV1 receptor
cancer pain
osteoarthritic pain
incontinence
title Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive Afferents
title_full Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive Afferents
title_fullStr Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive Afferents
title_full_unstemmed Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive Afferents
title_short Resiniferatoxin: Nature’s Precision Medicine to Silence TRPV1-Positive Afferents
title_sort resiniferatoxin nature s precision medicine to silence trpv1 positive afferents
topic resiniferatoxin
capsaicin
TRPV1 receptor
cancer pain
osteoarthritic pain
incontinence
url https://www.mdpi.com/1422-0067/24/20/15042
work_keys_str_mv AT arpadszallasi resiniferatoxinnaturesprecisionmedicinetosilencetrpv1positiveafferents