Transient receptor potential vanilloid 1 (TRPV1) antagonism in patients with refractory chronic cough: a double-blind randomized controlled trial

J Allergy Clin Immunol. 2014 Jul;134(1):56-62. doi: 10.1016/j.jaci.2014.01.038. Epub 2014 Mar 22.

Abstract

Background: Inhalation of capsaicin, the extract of hot chili peppers, induces coughing in both animals and human subjects through activation of transient receptor potential vanilloid 1 (TRPV1) on airway sensory nerves. Therefore the TRPV1 receptor is an attractive target for the development of antitussive agents.

Objective: We sought to assess the antitussive effect of TRPV1 antagonism in patients with refractory chronic cough.

Methods: Twenty-one subjects with refractory chronic cough (>8 weeks) attending a specialist clinic were recruited to a randomized, double-blind, placebo-controlled crossover trial assessing a TRPV1 antagonist (SB-705498). Cough reflex sensitivity to capsaicin (concentration of capsaicin inducing at least 5 coughs) and 24-hour cough frequency were coprimary end points assessed after a single dose of SB-705498 (600 mg) and matched placebo. Cough severity and urge to cough were reported on visual analog scales, and cough-specific quality of life data were also collected.

Results: Treatment with SB-705498 produced a significant improvement in cough reflex sensitivity to capsaicin at 2 hours and a borderline significant improvement at 24 hours compared with placebo (adjusted mean difference of +1.3 doubling doses at 2 hours [95% CI, +0.3 to +2.2; P = .0049] and +0.7 doubling doses at 24 hours [95% CI, +0.0 to +1.5; P = .0259]). However, 24-hour objective cough frequency was not improved compared with placebo. Patient-reported cough severity, urge to cough, and cough-specific quality of life similarly suggested no effect of SB-705498.

Conclusion: This study raises important questions about both the role of TRVP1-mediated mechanisms in patients with refractory chronic cough and also the predictive value of capsaicin challenge testing in the assessment of novel antitussive agents.

Keywords: Cough; capsaicin; cough sounds; sensory nerves; transient receptor potential vanilloid 1.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Inhalation
  • Adult
  • Aged
  • Animals
  • Antitussive Agents / therapeutic use*
  • Capsaicin
  • Chronic Disease
  • Cough / chemically induced
  • Cough / drug therapy*
  • Cough / genetics
  • Cough / physiopathology
  • Cross-Over Studies
  • Double-Blind Method
  • Female
  • Gene Expression
  • Humans
  • Male
  • Middle Aged
  • Pyrrolidines / therapeutic use*
  • Quality of Life
  • Severity of Illness Index
  • TRPV Cation Channels / antagonists & inhibitors*
  • TRPV Cation Channels / genetics
  • Treatment Outcome
  • Urea / analogs & derivatives*
  • Urea / therapeutic use

Substances

  • Antitussive Agents
  • Pyrrolidines
  • SB 705498
  • TRPV Cation Channels
  • TRPV1 protein, human
  • Urea
  • Capsaicin