Phosphodiesterase type 5 (PDE5) selectively hydrolyses the second messenger cyclic 3´-5´guanosine monophosphate (cGMP) into 5'-GMP, thereby regulating its intracellular concentrations. Dysregulation of the cGMP-dependent pathway plays a significant role in various cardiovascular diseases.
Therefore, its modulation by drugs, such as PDE5 inhibitors, may represent an effective therapeutic approach. There are currently four PDE5 inhibitors available for the treatment of erectile dysfunction: sildenafil, vardenafil, tadalafil, and avanafil. Sildenafil and tadalafil also received Food and Drug Administration approval for the treatment of pulmonary arterial hypertension. This review summarises the pharmacological aspects and clinical potential of PDE5 inhibition in the treatment of myocardial ischemia/reperfusion injury and heart failure.
British journal of pharmacology. 2017 Feb 18 [Epub ahead of print]
Sevil Korkmaz-Icöz, Tamás Radovits, Gábor Szabó
Department of Cardiac Surgery, Heidelberg University Hospital, Heidelberg, Germany., Heart and Vascular Center, Semmelweis University, Budapest, Hungary.