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Finally a promising analgesic signal in a long-awaited new class of drugs: TRPV1 antagonist mavatrep in patients with osteoarthritis (OA)

Finally a promising analgesic signal in a long-awaited new class of drugs: TRPV1 antagonist... In this issue of Scandinavian Journal of Pain, Mayorga et al. report positive efficacy data of mavatrep, a transient receptor potential vanilloid subtype 1 (TRPV1) antagonist, in OA pain [1]. A positive signal of efficacy has been reported previously in dental extraction pain [2], but this is the first report of a signal of efficacy with a TRPV1 antagonist in a chronic pain condition.1What is transient receptor potential vanilloid subtype 1 (TRPV1)?TRPV1 is a cation channel located on peripheral nociceptive fibres, but also in areas involved in nociception in the central nervous system [3,4]. The receptor is activated by heat, capsaicin and low pH and the activity is regulated by inflammatory regulators [5]. The TRPV1 receptor acts as a polymodal signal detector and may be influenced by several simultaneous stimuli, e.g. the thermal activation curve for the TRPV1 receptor is shifted to the left by capsaicin [6].2Difficulties in developing this class of analgesic drugs – the TRPVl-anatagonistsBased on these properties, indicating a pivotal role for TRPV1 in nociception, many TRPV1 antagonists have been developed displaying efficacy in animal models of a variety of pain conditions, like inflammatory, osteoarthritis, and neuropathic pain models [5,7]. The clinical development of this class http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Scandinavian Journal of Pain de Gruyter

Finally a promising analgesic signal in a long-awaited new class of drugs: TRPV1 antagonist mavatrep in patients with osteoarthritis (OA)

Karlsten, Rolf
Scandinavian Journal of Pain , Volume 17 (1): 2 – Oct 1, 2017
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Publisher
de Gruyter
Copyright
© 2017 Scandinavian Association for the Study of Pain
ISSN
1877-8860
eISSN
1877-8879
DOI
10.1016/j.sjpain.2017.08.015
Publisher site
See Article on Publisher Site

Abstract

In this issue of Scandinavian Journal of Pain, Mayorga et al. report positive efficacy data of mavatrep, a transient receptor potential vanilloid subtype 1 (TRPV1) antagonist, in OA pain [1]. A positive signal of efficacy has been reported previously in dental extraction pain [2], but this is the first report of a signal of efficacy with a TRPV1 antagonist in a chronic pain condition.1What is transient receptor potential vanilloid subtype 1 (TRPV1)?TRPV1 is a cation channel located on peripheral nociceptive fibres, but also in areas involved in nociception in the central nervous system [3,4]. The receptor is activated by heat, capsaicin and low pH and the activity is regulated by inflammatory regulators [5]. The TRPV1 receptor acts as a polymodal signal detector and may be influenced by several simultaneous stimuli, e.g. the thermal activation curve for the TRPV1 receptor is shifted to the left by capsaicin [6].2Difficulties in developing this class of analgesic drugs – the TRPVl-anatagonistsBased on these properties, indicating a pivotal role for TRPV1 in nociception, many TRPV1 antagonists have been developed displaying efficacy in animal models of a variety of pain conditions, like inflammatory, osteoarthritis, and neuropathic pain models [5,7]. The clinical development of this class

Journal

Scandinavian Journal of Pain – de Gruyter

Published: Oct 1, 2017

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