Drug intelligence / Profile preview

spironolactone + vitamin D3

Development stage
Preclinical
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Spironolactone + vitamin D3 is a combination of two agents: **spironolactone**, a potassium-sparing diuretic and mineralocorticoid receptor antagonist, and **vitamin D3** (cholecalciferol), a fat-soluble vitamin involved in calcium homeostasis and bone metabolism. Spironolactone acts by antagonizing the effects of aldosterone at the mineralocorticoid receptor, leading to increased sodium and water excretion while sparing potassium. Vitamin D3 is converted in the body to its active form, which regulates calcium absorption and modulates immune function. This combination has been shown in preclinical studies to modulate inflammation, enhance wound healing, and change macrophage polarization when applied in the context of skin injury; its clinical use as a fixed pharmaceutical combination is not established, though both agents are approved as monotherapies for various indications[1][4].

02

Targets

GR (Glucocorticoid receptor)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)VDR (Vitamin D receptor)

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