Esaxerenone, a novel nonsteroidal mineralocorticoid receptor blocker (MRB) in hypertension and chronic kidney disease

Crystal structure of the mineralocorticoid receptor ligand‐binding domain in complex with a potent and selective nonsteroidal blocker, esaxerenone (CS‐3150)

(2020) Mizuki Takahashi et al.   FEBS LETTERS

Effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone (CS-3150), on blood pressure and renal injury in high salt-treated type 2 diabetic mice

(2019) Abdus Sattar Bhuiyan et al.   HYPERTENSION RESEARCH

Esaxerenone: First Global Approval

(2019) Sean Duggan   DRUGS

Absolute Bioavailability of Esaxerenone and Food Effects on its Pharmacokinetics After a Single Oral Dose in Healthy Japanese Subjects: An Open-Label Crossover Study

(2019) Akifumi Kurata et al.   ADVANCES IN THERAPY

Efficacy and safety of esaxerenone (CS-3150) for the treatment of essential hypertension: a phase 2 randomized, placebo-controlled, double-blind study

(2019) Sadayoshi Ito et al.   JOURNAL OF HUMAN HYPERTENSION

Efficacy and Safety of Esaxerenone (CS-3150) for the Treatment of Type 2 Diabetes with Microalbuminuria

(2019) Sadayoshi Ito et al.   Clinical Journal of the American Society of Nephrology

Efficacy and safety of dosage-escalation of low-dosage esaxerenone added to a RAS inhibitor in hypertensive patients with type 2 diabetes and albuminuria: a single-arm, open-label study

(2019) Hiroshi Itoh et al.   HYPERTENSION RESEARCH

Long-term phase 3 study of esaxerenone as mono or combination therapy with other antihypertensive drugs in patients with essential hypertension

(2019) Hiromi Rakugi et al.   HYPERTENSION RESEARCH

Role of Aldosterone and Mineralocorticoid Receptor in Cardiovascular Aging

(2019) Stefania Gorini et al.   Frontiers in Endocrinology

Pharmacokinetics and Safety of Single-Dose Esaxerenone in Japanese Subjects with Mild to Moderate Hepatic Impairment

(2019) Akifumi Kurata et al.   ADVANCES IN THERAPY

Double-Blind Randomized Phase 3 Study Comparing Esaxerenone (CS-3150) and Eplerenone in Patients With Essential Hypertension (ESAX-HTN Study)

(2019) Sadayoshi Ito et al.   HYPERTENSION

Single- and multiple-dose escalation study to assess pharmacokinetics, pharmacodynamics and safety of oral esaxerenone in healthy Japanese subjects

(2018) Manabu Kato et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Independent regulation of renin–angiotensin–aldosterone system in the kidney

(2018) Akira Nishiyama et al.   Clinical and Experimental Nephrology

The use of a novel non-steroidal mineralocorticoid receptor antagonist finerenone for the treatment of chronic heart failure

(2018) Hui Pei et al.   MEDICINE

Preclinical pharmacology of AZD9977: A novel mineralocorticoid receptor modulator separating organ protection from effects on electrolyte excretion

(2018) Krister Bamberg et al.   PLoS One

Pharmacokinetics, Metabolism, and Excretion of [14C]Esaxerenone, a Novel Mineralocorticoid Receptor Blocker in Humans

(2018) Makiko Yamada et al.   DRUG METABOLISM AND DISPOSITION

Pathophysiological mechanisms of mineralocorticoid receptor-dependent cardiovascular and chronic kidney disease

(2018) Akira Nishiyama   HYPERTENSION RESEARCH

Effects of the novel nonsteroidal mineralocorticoid receptor blocker, esaxerenone (CS-3150), on blood pressure and urinary angiotensinogen in low-renin Dahl salt-sensitive hypertensive rats

(2018) Lei Li et al.   HYPERTENSION RESEARCH

Aldosterone and Mineralocorticoid Receptors—Physiology and Pathophysiology

(2017) John Funder   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of research and development

(2017) Peter Kolkhof et al.   JOURNAL OF ENDOCRINOLOGY

Spironolactone

(2017) Laura Carone et al.   JOURNAL OF PAIN AND SYMPTOM MANAGEMENT

Mineralocorticoid receptor antagonists—pharmacodynamics and pharmacokinetic differences

(2016) Jun Yang et al.   CURRENT OPINION IN PHARMACOLOGY

Steroidal and Nonsteroidal Mineralocorticoid Receptor Antagonists Cause Differential Cardiac Gene Expression in Pressure Overload-induced Cardiac Hypertrophy

(2016) Jana Grune et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys

(2016) Makiko Yamada et al.   XENOBIOTICA

Non-steroidal mineralocorticoid receptor antagonism for the treatment of cardiovascular and renal disease

(2015) Peter Bramlage et al.   EUROPEAN JOURNAL OF HEART FAILURE

Pharmacological profile of CS-3150, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist

(2015) Kiyoshi Arai et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

CS-3150, a novel non-steroidal mineralocorticoid receptor antagonist, prevents hypertension and cardiorenal injury in Dahl salt-sensitive hypertensive rats

(2015) Kiyoshi Arai et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Safety profile of mineralocorticoid receptor antagonists: Spironolactone and eplerenone

(2015) Mitja Lainscak et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

Finerenone, a Novel Selective Nonsteroidal Mineralocorticoid Receptor Antagonist Protects From Rat Cardiorenal Injury

(2014) Peter Kolkhof et al.   JOURNAL OF CARDIOVASCULAR PHARMACOLOGY

Discovery of BAY 94-8862: A Nonsteroidal Antagonist of the Mineralocorticoid Receptor for the Treatment of Cardiorenal Diseases

(2012) Lars Bärfacker et al.   ChemMedChem

Mineralocorticoid Receptor Antagonists for the Treatment of Hypertension and Diabetic Nephropathy

(2012) David W. Piotrowski   JOURNAL OF MEDICINAL CHEMISTRY

Mechanisms of ligand specificity of the mineralocorticoid receptor

(2011) Peter J Fuller et al.   JOURNAL OF ENDOCRINOLOGY

Aldosterone antagonists are underused by clinicians

(2010) Jane-Lise Samuel et al.   Nature Reviews Cardiology