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The capsaicin receptor, TRPV1, has been one of the most extensively studied molecules in sensory research. Its contribution to the sensation of pain in numerous pre-clinical inflammatory and neuropathic paradigms has been well-established and expression analysis suggests a potential role clinically in pain and bladder conditions. The field has now reached an exciting point in time with the development of a number of high quality TRPV1 antagonist drug candidates and the release of clinical data. What has become apparent from this work is that inhibition of TRPV1 function brings with it the potential liabilities of increased body temperature and altered thermal perception. However, there is cause for optimism because it appears that not all antagonists have the same properties and compounds can be identified that lack significant on-target side-effects whilst retaining efficacy, at least pre-clinically. What is perhaps now more critical to address is the question of how effective the analgesia provided by a TRPV1 antagonist will be. Although tantalizing clinical data showing effects on experimentally-induced pain or pain following molar extraction have been reported, no clear efficacy in a chronic pain condition has yet been demonstrated making it difficult to perform an accurate risk-benefit analysis for TRPV1 antagonists. Here we provide an overview of some of the most advanced clinical candidates and discuss the approaches being taken to avoid the now well established on-target effects of TRPV1 antagonists.

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