Esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker (MRB) in hypertension and chronic kidney disease.
Journal
Journal of human hypertension
ISSN: 1476-5527
Titre abrégé: J Hum Hypertens
Pays: England
ID NLM: 8811625
Informations de publication
Date de publication:
02 2021
02 2021
Historique:
received:
11
03
2020
accepted:
30
06
2020
revised:
22
05
2020
pubmed:
15
7
2020
medline:
27
8
2021
entrez:
15
7
2020
Statut:
ppublish
Résumé
The steroidal mineralocorticoid receptor (MR) antagonists, spironolactone and eplerenone, decrease blood pressure, and attenuate the progression of chronic kidney disease (CKD). However, their use is limited by the fear of inducing hyperkalemia, gynecomastia, impotence, and amenorrhea. Esaxerenone is a novel nonsteroidal MR blocker (MRB) that has been recently developed. In vitro studies have revealed that esaxerenone has a high potency and selectivity for MR compared with spironolactone and eplerenone. Further studies have shown that esaxerenone elicits a strong blood pressure-lowering effect in hypertensive animals. Following the results from phase III clinical trials that esaxerenone is an effective and well-tolerated MRB in Japanese hypertensive patients, esaxerenone became clinically available in Japan from May 2019 for hypertensive patients. Thus, esaxerenone is a promising treatment option for patients with hypertension. In addition, both preclinical studies and phase II clinical trials have shown that esaxerenone elicits renoprotection independent of its antihypertensive effect. Recently, a phase III clinical trial (ESAX-DN study) has also demonstrated the safety and efficacy of esaxerenone in patients with type 2 diabetes and microalbuminuria. These data support future clinical development of esaxerenone for the treatment of renal disease.
Identifiants
pubmed: 32661269
doi: 10.1038/s41371-020-0377-6
pii: 10.1038/s41371-020-0377-6
doi:
Substances chimiques
Mineralocorticoid Receptor Antagonists
0
Pyrroles
0
Receptors, Mineralocorticoid
0
Sulfones
0
Spironolactone
27O7W4T232
esaxerenone
N62TGJ04A1
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
148-156Références
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