Last reviewed · How we verify
Inspra (EPLERENONE)
Inspra works by blocking the action of aldosterone, a hormone that can cause the body to retain too much salt and water.
Inspra (Eplerenone) is a small molecule aldosterone antagonist that targets the mineralocorticoid receptor. It was originally developed by GD Searle LLC and is now owned by Upjohn. Inspra is FDA-approved for the treatment of chronic heart failure following myocardial infarction and hypertensive disorders. The drug is off-patent and has multiple generic manufacturers. Key safety considerations include monitoring of potassium levels and potential increased risk of hyperkalemia.
At a glance
| Generic name | EPLERENONE |
|---|---|
| Sponsor | Upjohn |
| Drug class | Aldosterone Antagonist [EPC] |
| Target | Mineralocorticoid receptor |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
| First approval | 2002 |
Mechanism of action
Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, component of the renin-angiotensin-aldosterone-system (RAAS). Aldosterone synthesis, which occurs primarily in the adrenal gland, is modulated by multiple factors, including angiotensin II and non-RAAS mediators such as adrenocorticotropic hormone (ACTH) and potassium. Aldosterone binds to mineralocorticoid receptors in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, blood vessels, and brain) tissues and increases blood pressure through induction of sodium reabsorption and possibly other mechanisms. Eplerenone has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to human mineraloc
Approved indications
- Chronic Heart Failure Following Myocardial Infarction
- Hypertensive disorder
Common side effects
- Cardiac failure
- Acute kidney injury
- Hyperkalaemia
- Ventricular tachycardia
- Hypotension
- Oedema peripheral
- Ejection fraction decreased
- Rales
- N-terminal prohormone brain natriuretic peptide increased
- Mitral valve incompetence
- Atrial fibrillation
- Glomerular filtration rate decreased
Drug interactions
- amprenavir
- aprepitant
- atazanavir
- boceprevir
- ciprofloxacin
- conivaptan
- darunavir
- diltiazem
- erythromycin
- fluconazole
- fosamprenavir
- imatinib
Key clinical trials
- Stratified Medicine of Eplerenone in Acute Myocardial Infarction or Injury and no Obstructive Coronary Arteries. (PHASE2)
- Swedish Cardiac And Renal Failure Study-1 (PHASE2)
- Vascular Effects of High-Salt After Preeclampsia (EARLY_PHASE1)
- MR and Inflammation After Preeclampsia (EARLY_PHASE1)
- A Clinical Study Using FAPI-PET Imaging to Assess the Postoperative Effects of TAVI in Patients With Aortic Stenosis (NA)
- Mineralocorticoid Receptor, Coronary Microvascular Function, and Cardiac Efficiency in Hypertension (PHASE4)
- Cardiac Effects of Mineralocorticoid Receptor Antagonism After Preeclampsia (PHASE2)
- Tissue K+ in Primary Hyperaldosteronism
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Inspra CI brief — competitive landscape report
- Inspra updates RSS · CI watch RSS
- Upjohn portfolio CI