tezosentan

Tezosentan is a small molecule intravenous dual endothelin receptor antagonist with high affinity for both endothelin A (ETA) and endothelin B (ETB) receptors, showing greater potency for ETA. It was originally developed by Actelion as a vasodilator to treat acute heart failure and pulmonary arterial hypertension. Tezosentan works by blocking the effects of endothelin‑1 (ET1), a potent vasoconstrictor, thereby dilating blood vessels, improving cardiac output, reducing pulmonary capillary wedge pressure, and decreasing systemic vascular resistance. Despite promising hemodynamic effects in early studies—including increased cardiac power index and reduced peripheral resistance—clinical trials did not demonstrate significant benefit in relieving dyspnea or preventing cardiovascular events in acute heart failure patients. Tezosentan has also been investigated for potential anticancer properties due to its ability to inhibit ET receptors involved in tumor cell proliferation and drug resistance[1][3][4][6][7].

Brand names

Veletri

Other names

tezosentan [INN]N-(2-(2-(2H-tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide180384-57-0