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Transient receptor potential channel modulators as pharmacological treatments for lower urinary tract symptoms (LUTS): myth or reality?
BJU Int. 2015 May; 115(5):686-97.BI

Abstract

Transient receptor potential (TRP) channels belong to the most intensely pursued drug targets of the last decade. These ion channels are considered promising targets for the treatment of pain, hypersensitivity disorders and lower urinary tract symptoms (LUTS). The aim of the present review is to discuss to what extent TRP channels have adhered to their promise as new pharmacological targets in the lower urinary tract (LUT) and to outline the challenges that lie ahead. TRP vanilloid 1 (TRPV1) agonists have proven their efficacy in the treatment of neurogenic detrusor overactivity (DO), albeit at the expense of prolonged adverse effects as pelvic 'burning' pain, sensory urgency and haematuria. TRPV1 antagonists have been very successful in preclinical studies to treat pain and DO. However, clinical trials with the first generation TRPV1 antagonists were terminated early due to hyperthermia, a serious, on-target, side-effect. TRP vanilloid 4 (TRPV4), TRP ankyrin 1 (TRPA1) and TRP melastatin 8 (TRPM8) have important sensory functions in the LUT. Antagonists of these channels have shown their potential in pre-clinical studies of LUT dysfunction and are awaiting clinical validation.

Authors+Show Affiliations

Laboratory of Experimental Urology, Department of Development and Regeneration, KU Leuven, Leuven, Belgium; University Hospitals Leuven, Leuven, Belgium; TRP Research Platform Leuven (TRPLe), Leuven, Belgium.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

25060242

Citation

Deruyver, Yves, et al. "Transient Receptor Potential Channel Modulators as Pharmacological Treatments for Lower Urinary Tract Symptoms (LUTS): Myth or Reality?" BJU International, vol. 115, no. 5, 2015, pp. 686-97.
Deruyver Y, Voets T, De Ridder D, et al. Transient receptor potential channel modulators as pharmacological treatments for lower urinary tract symptoms (LUTS): myth or reality? BJU Int. 2015;115(5):686-97.
Deruyver, Y., Voets, T., De Ridder, D., & Everaerts, W. (2015). Transient receptor potential channel modulators as pharmacological treatments for lower urinary tract symptoms (LUTS): myth or reality? BJU International, 115(5), 686-97. https://doi.org/10.1111/bju.12876
Deruyver Y, et al. Transient Receptor Potential Channel Modulators as Pharmacological Treatments for Lower Urinary Tract Symptoms (LUTS): Myth or Reality. BJU Int. 2015;115(5):686-97. PubMed PMID: 25060242.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transient receptor potential channel modulators as pharmacological treatments for lower urinary tract symptoms (LUTS): myth or reality? AU - Deruyver,Yves, AU - Voets,Thomas, AU - De Ridder,Dirk, AU - Everaerts,Wouter, Y1 - 2015/01/21/ PY - 2014/7/26/entrez PY - 2014/7/26/pubmed PY - 2015/6/20/medline KW - LUTS KW - TRP channel KW - TRPV1 KW - TRPV4 KW - afferent nerve KW - detrusor overactivity KW - urothelium SP - 686 EP - 97 JF - BJU international JO - BJU Int VL - 115 IS - 5 N2 - Transient receptor potential (TRP) channels belong to the most intensely pursued drug targets of the last decade. These ion channels are considered promising targets for the treatment of pain, hypersensitivity disorders and lower urinary tract symptoms (LUTS). The aim of the present review is to discuss to what extent TRP channels have adhered to their promise as new pharmacological targets in the lower urinary tract (LUT) and to outline the challenges that lie ahead. TRP vanilloid 1 (TRPV1) agonists have proven their efficacy in the treatment of neurogenic detrusor overactivity (DO), albeit at the expense of prolonged adverse effects as pelvic 'burning' pain, sensory urgency and haematuria. TRPV1 antagonists have been very successful in preclinical studies to treat pain and DO. However, clinical trials with the first generation TRPV1 antagonists were terminated early due to hyperthermia, a serious, on-target, side-effect. TRP vanilloid 4 (TRPV4), TRP ankyrin 1 (TRPA1) and TRP melastatin 8 (TRPM8) have important sensory functions in the LUT. Antagonists of these channels have shown their potential in pre-clinical studies of LUT dysfunction and are awaiting clinical validation. SN - 1464-410X UR - https://www.unboundmedicine.com/medline/citation/25060242/Transient_receptor_potential_channel_modulators_as_pharmacological_treatments_for_lower_urinary_tract_symptoms__LUTS_:_myth_or_reality L2 - https://doi.org/10.1111/bju.12876 DB - PRIME DP - Unbound Medicine ER -