Drug intelligence / Profile preview

spironolactone + dexamethasone

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

Overview

Spironolactone + dexamethasone is a combination of two small molecule drugs, each with distinct mechanisms of action. Spironolactone is a potassium-sparing diuretic and mineralocorticoid receptor antagonist, primarily used to treat conditions such as hypertension, heart failure, edema associated with liver cirrhosis or nephrotic syndrome, and hyperaldosteronism. It also has antiandrogenic effects and is sometimes used off-label for hirsutism in women[9][7]. Dexamethasone is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties. The combination has been studied in clinical settings such as non-tumorous hyperandrogenism (e.g., hirsutism) and more recently in COVID-19 hospitalized patients to assess potential additive benefits on disease severity by combining mineralocorticoid receptor blockade (spironolactone) with glucocorticoid-mediated cortisol suppression (dexamethasone)[1][3][5]. Clinical trials have shown the combination to be safe but not significantly superior to monotherapy for some indications; however, it may reduce certain biomarkers like D-dimer and aldosterone in COVID-19[3][5].

Other names
Spironolactone and Dexamethasone in Patients Hospitalized With Moderate-to-severe COVID-19
02

Targets

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

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