NVA237, a long-acting muscarinic antagonist, as an emerging therapy for chronic obstructive pulmonary disease

Ther Adv Respir Dis. 2011 Jun;5(3):163-73. doi: 10.1177/1753465811406001. Epub 2011 Apr 20.

Abstract

Bronchodilation with a long-acting muscarinic antagonist (LAMA) or long-acting β(2)-agonist is central to the management of chronic obstructive pulmonary disease (COPD). Tiotropium, the first LAMA available for use in COPD, has been shown to be an effective bronchodilator and is generally safe and well tolerated. However, tiotropium has limitations that include a high incidence of dry mouth, slow onset of action and, in some studies, a part of the patient population did not achieve clinically significant bronchodilation. It also remains unclear whether tiotropium reduces progressive deterioration of lung function in patients with COPD. An ideal LAMA would provide clinically meaningful bronchodilation, deliver symptom relief, prevent disease progression, improve exercise tolerance and health status, prevent and treat complications and exacerbations and reduce mortality risk. A 24-h duration of action, rapid onset of action and a good safety and tolerability profile are also desirable. The once-daily LAMA, NVA237 (glycopyrronium bromide), may meet some of these characteristics. NVA237 has high selectivity for the muscarinic type-3 (M(3)) receptor which might potentially result in a higher therapeutic index than tiotropium, which is less selective for M(3). Phase II studies showed that NVA237 once daily provides clinically significant 24-h bronchodilation with a rapid onset of action and a favourable safety and tolerability profile. Phase III studies are ongoing that will assess the long-term safety and efficacy of NVA237.

Publication types

  • Review

MeSH terms

  • Bronchodilator Agents / adverse effects
  • Bronchodilator Agents / pharmacology
  • Bronchodilator Agents / therapeutic use
  • Delayed-Action Preparations
  • Glycopyrrolate / adverse effects
  • Glycopyrrolate / pharmacology
  • Glycopyrrolate / therapeutic use*
  • Humans
  • Muscarinic Antagonists / adverse effects
  • Muscarinic Antagonists / pharmacology
  • Muscarinic Antagonists / therapeutic use*
  • Pulmonary Disease, Chronic Obstructive / drug therapy*
  • Pulmonary Disease, Chronic Obstructive / physiopathology
  • Receptor, Muscarinic M3 / antagonists & inhibitors
  • Scopolamine Derivatives / adverse effects
  • Scopolamine Derivatives / pharmacology
  • Scopolamine Derivatives / therapeutic use
  • Tiotropium Bromide

Substances

  • Bronchodilator Agents
  • Delayed-Action Preparations
  • Muscarinic Antagonists
  • Receptor, Muscarinic M3
  • Scopolamine Derivatives
  • Glycopyrrolate
  • Tiotropium Bromide