Drug intelligence / Profile preview

canrenoate + eplerenone + spironolactone

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of three mineralocorticoid receptor antagonists (MRAs): canrenoate, eplerenone, and spironolactone. All three are potassium-sparing diuretics that act primarily by antagonizing the effects of aldosterone at the mineralocorticoid receptor in the distal renal tubules. This leads to increased excretion of sodium and water while retaining potassium, making them effective for treating conditions such as heart failure, hypertension, and edema associated with liver or kidney disease. Spironolactone also has antiandrogenic properties; canrenoate is a prodrug that is converted to active metabolites including canrenone; eplerenone is more selective for the mineralocorticoid receptor with fewer endocrine side effects compared to spironolactone. These agents are used individually in clinical practice but there is no evidence or approval for their combined use as a single pharmaceutical product.

02

Targets

PR (Progesterone receptor)GR (Glucocorticoid receptor)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)ER (Estrogen receptor)

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