Drug intelligence / Profile preview

sitaxsentan + sildenafil

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Sitaxsentan + sildenafil is a combination therapy consisting of two small molecule drugs used in the management of pulmonary arterial hypertension (PAH). Sitaxsentan is a selective endothelin-A receptor antagonist that blocks the vasoconstrictive and proliferative effects of endotheelin-1 on vascular smooth muscle. Sildenafil is a phosphodiesterase-5 inhibitor that increases cyclic GMP levels, leading to vasodilation in the pulmonary vasculature. The combination targets two distinct but complementary pathways involved in PAH pathogenesis—endothelin-mediated vasoconstriction and impaired nitric oxide signaling. Preclinical studies and clinical trials have shown that this combination can more effectively prevent or limit increases in pulmonary vascular resistance (PVR) and vascular remodeling compared to monotherapy with either agent[1][4][5]. However, controlled safety/efficacy data for this specific combination are limited, and development was discontinued before regulatory approval[3][6].

Other names
sitaxsentan and sildenafilsitaxsentan plus sildenafil
02

Targets

PDE6 (Phosphodiesterase 6)EDNRB (Endothelin receptor type B)EDNRA (Endothelin receptor type A)PDE5 (Phosphodiesterase 5A)

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