The next generation of PDE4 inhibitors.

A number of highly potent PDE4 inhibitors are being developed for the treatment of asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis and Crohn's disease. Cilomilast (Ariflo, SB 207499, SmithKline Beecham), the most advanced member of the class in Phase III clinical trials, was reported to have a limited therapeutic window. Other inhibitors with improved profiles in preclinical models are entering into (or are in) clinical trials. The recent developments in understanding PDE4 catalysis, inhibitor binding and their emetic response should facilitate the design of the next generation of PDE4 inhibitors.
AuthorsZ Huang, Y Ducharme, D Macdonald, A Robichaud
JournalCurrent opinion in chemical biology (Curr Opin Chem Biol) Vol. 5 Issue 4 Pg. 432-8 (Aug 2001) ISSN: 1367-5931 [Print] England
PMID11470607 (Publication Type: Journal Article, Review)
Chemical References
  • Antiemetics
  • Cyclohexanecarboxylic Acids
  • Nitriles
  • Phosphodiesterase Inhibitors
  • Cilomilast
  • 3',5'-Cyclic-AMP Phosphodiesterases
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • 3',5'-Cyclic-AMP Phosphodiesterases (antagonists & inhibitors)
  • Antiemetics (pharmacology)
  • Catalysis
  • Cyclic Nucleotide Phosphodiesterases, Type 4
  • Cyclohexanecarboxylic Acids (pharmacology, therapeutic use)
  • Humans
  • Nitriles
  • Phosphodiesterase Inhibitors (pharmacology, therapeutic use)

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