Soluble guanylate cyclase stimulator explained

Soluble guanylate cyclase (sGC) stimulators are a class of drugs developed to treat heart failure, pulmonary hypertension, and other diseases. The first-in-class medication was riociguat, approved in 2013 for pulmonary hypertension.[1] They have also been investigated for hypertension, systemic sclerosis, and sickle cell disease.

Background

In 1998, the role of nitric oxide (NO) in cardiovascular disease received the Nobel Prize in Physiology. Although NO is still used to treat angina, its side effects, potential for tolerance, short duration of action, and narrow therapeutic index limit its therapeutic use.[2] PDE5 inhibitors increase NO and are approved for erectile dysfunction, pulmonary arterial hypertension (PAH), and benign prostatic hyperplasia, but they are less effective in patients for whom NO production is suppressed, such as people with diabetes or obesity. Soluble guanylate cyclase is one of the downstream targets of NO, but the stimulators operate independently of it.[3] sGC activators, another experimental class of drugs, may be more effective than stimulators when oxidative stress is high.[3]

The drugs are also considered to possibly have the potential to treat kidney disease, lung fibrosis, scleroderma, and sickle cell disease.[4] [3]

List of drugs

FDA approved

Investigational

Notes and References

  1. Sandner . Peter . Vakalopoulos . Alexandros . Hahn . Michael G. . Stasch . Johannes-Peter . Follmann . Markus . Soluble guanylate cyclase stimulators and their potential use: a patent review . Expert Opinion on Therapeutic Patents . 4 March 2021 . 31 . 3 . 203–222 . 10.1080/13543776.2021.1866538 . en . 1354-3776. free .
  2. Sandner . Peter . Zimmer . Daniel P. . Milne . G. Todd . Follmann . Markus . Hobbs . Adrian . Stasch . Johannes-Peter . Soluble Guanylate Cyclase Stimulators and Activators . Handbook of Experimental Pharmacology . 2021 . 264 . 355–394 . 10.1007/164_2018_197 . 0171-2004. free .
  3. Sandner . Peter . From molecules to patients: exploring the therapeutic role of soluble guanylate cyclase stimulators . Biological Chemistry . 1 July 2018 . 399 . 7 . 679–690 . 10.1515/hsz-2018-0155 . en . 1437-4315. free .
  4. Book: Stasch . Johannes-Peter . Evgenov . Oleg V. . Pharmacotherapy of Pulmonary Hypertension . 2013 . Springer . 978-3-642-38664-0 . 279–313 . en . Soluble Guanylate Cyclase Stimulators in Pulmonary Hypertension.
  5. Markham . Anthony . Duggan . Sean . Vericiguat: First Approval . Drugs . 1 April 2021 . 81 . 6 . 721–726 . 10.1007/s40265-021-01496-z . en . 1179-1950.
  6. Udelson . James E. . Lewis . Gregory D. . Shah . Sanjiv J. . Zile . Michael R. . Redfield . Margaret M. . Burnett . John . Parker . John . Seferovic . Jelena P. . Wilson . Phebe . Mittleman . Robert S. . Profy . Albert T. . Konstam . Marvin A. . Effect of Praliciguat on Peak Rate of Oxygen Consumption in Patients With Heart Failure With Preserved Ejection Fraction: The CAPACITY HFpEF Randomized Clinical Trial . JAMA . 20 October 2020 . 324 . 15 . 1522 . 10.1001/jama.2020.16641. free . 7576408 .
  7. Web site: PhD . Joana Carvalho . Cyclerion Suspends Development of Olinciguat for Sickle Cell Disease . sicklecellanemianews.com . 8 November 2023 . 20 October 2020.

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