Transient receptor potential vanilloid type 1 antagonists: A patent review (2011-2014)

Yoonji Lee, Sunhye Hong, Minghua Cui, Pankaz K. Sharma, Jeewoo Lee, Sun Choi

Research output: Contribution to journalReview articlepeer-review

62 Scopus citations


Introduction: Transient receptor potential vanilloid type 1 (TRPV1) is a nonselective cation channel that can be activated by noxious heat, low pH and vanilloid compounds such as capsaicin. Since TRPV1 acts as an integrator of painful stimuli, TRPV1 antagonists can be used as promising therapeutics for new types of analgesics.Areas covered: This review article covers the patents that claim TRPV1 antagonists and were published during 2011-2014. The patent evaluation is organized according to the applicant companies, and the representative chemical entities with important in vitro and in vivo data are summarized.Expert opinion: Many pharmaceutical companies showed promising results in the discovery of potent small molecule TRPV1 antagonists, and recently, a number of small molecule TRPV1 antagonists have been advanced into clinical trials. Unfortunately, several candidate molecules showed critical side effects such as hyperthermia and impaired noxious heat sensation in humans, leading to their withdrawal from clinical trials. Some TRPV1 antagonists patented in recent years (2011-2014) overcame these undesirable side effects, making the development of TRPV1 antagonists much more promising.

Original languageEnglish
Pages (from-to)291-318
Number of pages28
JournalExpert Opinion on Therapeutic Patents
Issue number3
StatePublished - 1 Mar 2015

Bibliographical note

Publisher Copyright:
© 2014 Informa UK, Ltd.


  • Capsaicin
  • TRPV1
  • TRPV1 antagonist
  • Transient receptor potential
  • VR1
  • VR1 antagonist
  • Vanilloid


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