Target intelligence / Profile preview

Cyclic GMP-specific 3',5'-cyclic phosphodiesterase (PDE5)

Target
PDE5
Molecular classification
Enzyme, Phosphodiesterase
01

Overview

Cyclic GMP-specific 3',5'-cyclic phosphodiesterase (abbreviated PDE5) is an enzyme responsible for the hydrolysis of cyclic guanosine monophosphate (cGMP) to 5'-GMP, thus regulating intracellular levels of cGMP. This enzyme is expressed in smooth muscle (including the corpus cavernosum, pulmonary vasculature, and to a lesser extent cardiac tissue), where it modulates vascular tone and contractility. PDE5 is the molecular target of widely used drugs for erectile dysfunction and pulmonary hypertension, such as sildenafil and tadalafil, due to its critical role in cGMP signaling. Inhibition of PDE5 leads to increased cGMP, promoting smooth muscle relaxation and vasodilation. Its dysregulation or altered activity has been implicated in cardiovascular disorders, right ventricular hypertrophy, and pulmonary vascular diseases.

Other names
Phosphodiesterase type 5PDE5AcGMP-specific phosphodiesterasePhosphodiesterase V
02

Mechanism of action

Inhibition of PDE5 increases intracellular cGMP, causing smooth muscle relaxation and vasodilation. Indirect reduction of cellular proliferation (vascular/cardiac smooth muscle). Modulation of contractile function in cardiac tissue.

03

Biological functions

Degradation of cyclic GMP (cGMP)Regulation of smooth muscle toneSignal transductionModulation of myocardial contractilityRegulation of vascular tone
04

Disease associations

Cardiovascular diseasePulmonary hypertensionErectile dysfunctionCardiac hypertrophyHeart failure
05

Safety considerations

Hypotension, especially in combination with nitratesHeadache, flushingVisual disturbances (due to cross-reactivity with PDE6, particularly for sildenafil and vardenafil)Priapism (rare)Hearing loss (rare)
06

Interacting drugs

Sildenafil (Viagra, Revatio)

4 more in the full profile.

07

Biomarkers

PDE5 expression levels in tissue (e.g., lung, heart, penis)cGMP plasma or tissue concentrations

Beyond the preview

Go deeper on Cyclic GMP-specific 3',5'-cyclic phosphodiesterase (PDE5).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Cyclic GMP-specific 3',5'-cyclic phosphodiesterase (PDE5).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call