Litcius/Paper detail

Novel non‐steroidal mineralocorticoid receptor antagonists in cardiorenal disease

Ulrich Kintscher, George L. Bakris, Peter Kolkhof

2021British Journal of Pharmacology158 citationsDOIOpen Access PDF

Abstract

Mineralocorticoid receptor antagonists (MRAs) are key agents in guideline-oriented drug therapy for cardiovascular diseases such as chronic heart failure with reduced ejection fraction and resistant hypertension. Currently available steroidal MRAs are efficacious in reducing morbidity and mortality; however, they can be associated with intolerable side effects including hyperkalaemia in everyday clinical practice. Recently, a new class of non-steroidal MRAs (including esaxerenone, AZD9977, apararenone, KBP-5074 and finerenone) have been developed with an improved benefit-risk profile and a novel indication for finerenone for diabetic kidney disease. To better understand the non-steroidal MRAs, this review provides information on the molecular pharmacology as well as relevant current preclinical and clinical data on cardiorenal outcomes. A comparative review of all compounds in the class is discussed with regard to clinical efficacy and safety as well as a perspective outlining their future use in clinical practice. LINKED ARTICLES: This article is part of a themed issue on Emerging Fields for Therapeutic Targeting of the Aldosterone-Mineralocorticoid Receptor Signaling Pathway. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.13/issuetoc.

Topics & Concepts

Mineralocorticoid receptorEplerenoneMRASMedicineGuidelinePharmacologyHeart failureKidney diseaseClinical trialIntensive care medicineAldosteroneBioinformaticsInternal medicineBiologyPathologyInduction motorQuantum mechanicsVoltagePhysicsVector controlHormonal Regulation and HypertensionIon Transport and Channel RegulationCardiovascular, Neuropeptides, and Oxidative Stress Research