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Details

Autor(en) / Beteiligte
Titel
Soluble GC stimulators and activators: Past, present and future
Ist Teil von
  • British journal of pharmacology, 2024-11, Vol.181 (21), p.4130-4151
Ort / Verlag
England: Blackwell Publishing Ltd
Erscheinungsjahr
2024
Quelle
MEDLINE
Beschreibungen/Notizen
  • The discovery of soluble GC (sGC) stimulators and sGC activators provided valuable tools to elucidate NO–sGC signalling and opened novel pharmacological opportunities for cardiovascular indications and beyond. The first‐in‐class sGC stimulator riociguat was approved for pulmonary hypertension in 2013 and vericiguat very recently for heart failure. sGC stimulators enhance sGC activity independent of NO and also act synergistically with endogenous NO. The sGC activators specifically bind to, and activate, the oxidised haem‐free form of sGC. Substantial research efforts improved on the first‐generation sGC activators such as cinaciguat, culminating in the discovery of runcaciguat, currently in clinical Phase II trials for chronic kidney disease and diabetic retinopathy. Here, we highlight the discovery and development of sGC stimulators and sGC activators, their unique modes of action, their preclinical characteristics and the clinical studies. In the future, we expect to see more sGC agonists in new indications, reflecting their unique therapeutic potential.
Sprache
Englisch
Identifikatoren
ISSN: 0007-1188, 1476-5381
eISSN: 1476-5381
DOI: 10.1111/bph.15698
Titel-ID: cdi_proquest_miscellaneous_2578769201

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