Korean J Androl.  2008 Jun;26(2):49-60.

Past, Present and Future of PDE5 Inhibitor

• Kim JJ
• Moon DG

Abstract

The phosphodiesterase type-5 inhibitors (PDE5-Is) sildenafil, vardenafil and tadalafil are widely used as first-line therapy for erectile dysfunction (ED). Since the approval of sildenafil in 1998, more than 40 million men worldwide have been successfully treated with PDE5-Is. Pharmacologically, the proven safety and high tolerance of PDE5-Is is an attractive tool to investigate further physiological functions of PDE5, for example the modulation of intracellular cyclic GMP (cGMP) pools. As cGMP is a key component of intracellular signaling this may provide novel therapeutic opportunities beyond ED even for indications in which chronic administration is necessary. The approval of sildenafil for the treatment of pulmonary hypertension in 2005 was a notable success in this area of research. A number of other potential new indications are currently in various phases of preclinical research and development. In recent years, extensive but very heterogeneous information has been published in this field. The aim of this review is to summarize existing preclinical and clinical knowledge and critically discuss the evidence to support potential future indications for PDE5 inhibitors.

Keyword

PDE5 Phosphodiesterases; Sildenafil; Valdenafil; Tadalafil; Erectile dysfunction

MeSH Terms

Carbolines
Cyclic GMP
Cyclic Nucleotide Phosphodiesterases, Type 5
Erectile Dysfunction
Humans
Hypertension, Pulmonary
Imidazoles
Male
Piperazines
Purines
Sulfones
Triazines
Sildenafil Citrate
Tadalafil
Vardenafil Dihydrochloride
Carbolines
Cyclic GMP
Cyclic Nucleotide Phosphodiesterases, Type 5
Imidazoles
Piperazines
Purines
Sulfones
Triazines