Soluble Guanylyl Cyclase Activators-Promising Therapeutic Option in the Pharmacotherapy of Heart Failure and Pulmonary Hypertension

Molecules. 2023 Jan 15;28(2):861. doi: 10.3390/molecules28020861.

Abstract

Endogenous nitric oxide (NO)-dependent vascular relaxation plays a leading role in the homeostasis of the cardiovascular, pulmonary, and vascular systems and organs, such as the kidneys, brain, and liver. The mechanism of the intracellular action of NO in blood vessels involves the stimulation of the activity of the soluble cytosolic form of guanylyl cyclase (soluble guanylyl cyclase, sGC), increasing the level of cyclic 3'-5'-guanosine monophosphate (cGMP) in smooth muscle and subsequent vasodilation. In recent years, a new group of drugs, soluble guanylyl cyclase stimulators, has found its way into clinical practice. Based on the CHEST-1 and PATENT-1 trials, riociguat was introduced into clinical practice for treating chronic thromboembolic pulmonary hypertension (CTEPH). In January 2021, the FDA approved the use of another drug, vericiguat, for the treatment of heart failure.

Keywords: chronic heart failure (CHF); guanylate cyclase (GC); pulmonary arterial hypertension (PAH); riociguat; vericiguat.

Publication types

  • Review

MeSH terms

  • Cyclic GMP
  • Guanylate Cyclase
  • Heart Failure* / drug therapy
  • Humans
  • Hypertension, Pulmonary* / drug therapy
  • Lung
  • Nitric Oxide / therapeutic use
  • Soluble Guanylyl Cyclase

Substances

  • Soluble Guanylyl Cyclase
  • Guanylate Cyclase
  • Cyclic GMP
  • Nitric Oxide

Grants and funding

This research received no external funding.