Roflumilast: a phosphodiesterase-4 inhibitor for the treatment of respiratory disease

Expert Opin Investig Drugs. 2006 Sep;15(9):1105-13. doi: 10.1517/13543784.15.9.1105.

Abstract

Asthma and chronic obstructive pulmonary disease (COPD) are two of the most common chronic diseases worldwide, yet the classes of drug licensed to treat these conditions have not changed appreciably over the last 20 years. Inhaled bronchodilators and glucocorticosteroids (often in combination) form the mainstay of therapy for respiratory diseases, but many patients (including the elderly and children) can have problems using inhaler devices and there is a clear preference for oral therapy. The prevalence of these respiratory diseases is on the increase worldwide and continues to represent an area of medicine with unmet medical needs, particularly in the treatment of COPD. Despite this increase, very few new classes of drugs have been introduced into clinical practice. Phosphodiesterase-4 inhibitors are a novel class of drugs in development for the treatment of respiratory diseases and there are a number of lead compounds in late clinical development. This review focuses on one of the most promising drugs in development, roflumilast, which has undergone extensive clinical evaluation.

Publication types

  • Review

MeSH terms

  • 3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
  • 3',5'-Cyclic-AMP Phosphodiesterases / metabolism*
  • Aminopyridines / adverse effects
  • Aminopyridines / chemistry
  • Aminopyridines / pharmacology
  • Aminopyridines / therapeutic use*
  • Animals
  • Benzamides / adverse effects
  • Benzamides / chemistry
  • Benzamides / pharmacology
  • Benzamides / therapeutic use*
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Cyclopropanes / adverse effects
  • Cyclopropanes / chemistry
  • Cyclopropanes / pharmacology
  • Cyclopropanes / therapeutic use
  • Humans
  • Phosphodiesterase Inhibitors / therapeutic use*
  • Respiration Disorders / drug therapy*
  • Respiration Disorders / enzymology*
  • Time Factors

Substances

  • Aminopyridines
  • Benzamides
  • Cyclopropanes
  • Phosphodiesterase Inhibitors
  • Roflumilast
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 4