Phosphodiesterase 5 inhibitors: current status and potential applications

• Published in: Nature reviews. Drug discovery Vol. 1; no. 9; pp. 674 - 682
• Main Author: Rotella, David P
• Format: Journal Article
• Language: English
• Published: England Nature Publishing Group 01.09.2002
• Subjects: Carbolines; Chemistry, Pharmaceutical; Clinical Trials as Topic; Enzymes; Erectile Dysfunction - drug therapy; Humans; Imidazoles - chemistry; Imidazoles - therapeutic use; Male; Pharmaceutical industry; Phosphodiesterase Inhibitors - chemistry; Phosphodiesterase Inhibitors - therapeutic use; Phosphoric Diester Hydrolases - genetics; Phosphoric Diester Hydrolases - physiology; Physiological aspects; Piperazines - chemistry; Piperazines - therapeutic use; Protein kinases; Purines; Sildenafil; Sildenafil Citrate; Structure-Activity Relationship; Sulfones; Tadalafil; Triazines; Vardenafil Dihydrochloride; United States
• ISSN: 1474-1776; 1474-1784; 1474-1784
• DOI: 10.1038/nrd893

Phosphodiesterase enzymes convert cyclic GMP and cyclic AMP to the corresponding nucleotide monophosphates. Phosphodiesterase 5 (PDE5) inhibition is now a widely accepted and efficacious therapeutic option for the treatment of erectile dysfunction in men, as a result of extensive clinical experience with sildenafil and other new PDE5 inhibitors. Research in the field continues at a substantial level to identify new, selective PDE5 inhibitors and to investigate their usefulness and activity in other areas. This review summarizes recent clinical trials with PDE5 inhibitors, advances in medicinal chemistry, and other activities and potential applications of this class of compounds.