Drug intelligence / Profile preview

ambrisentan + spironolactone

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

This combination involves **ambrisentan**, a selective endothelin receptor antagonist used primarily to treat pulmonary arterial hypertension (PAH), and **spironolactone**, an aldosterone receptor antagonist used for conditions like edema, hypertension, and heart failure. Ambrisentan works by preventing endothelin from constricting blood vessels, improving exercise capacity and hemodynamics in PAH patients. Spironolactone acts as a potassium-sparing diuretic by blocking aldosterone receptors, increasing sodium and water excretion while conserving potassium. The combination may offer benefits in treating PAH by addressing both endothelin-mediated vasoconstriction and aldosterone-related effects.

02

Targets

PR (Progesterone receptor)EDNRA (Endothelin receptor type A)EDNRB (Endothelin receptor type B)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)

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