rostafuroxin

Rostafuroxin is a small molecule antihypertensive drug, structurally classified as a digitoxigenin analog and 17-furanylsteroid derivative. It acts by selectively antagonizing the effects of endogenous ouabain (EO) and mutant adducin on the sodium-potassium ATPase (Na+/K+-ATPase), an enzyme critical for maintaining sodium and potassium gradients across cell membranes. By displacing ouabain from its binding site on Na+/K+-ATPase, rostafuroxin normalizes altered renal and vascular Na+/K+ pump function associated with certain forms of hypertension, particularly those linked to genetic variants in adducin or increased EO levels. This mechanism allows it to lower blood pressure without affecting normal physiological blood pressure regulation. Rostafuroxin has been investigated primarily for essential hypertension, especially in patients with specific gene variants that predispose them to salt-sensitive or resistant hypertension[1][3][5][6][7].

Other names

digitoxigenin derivative