Drug intelligence / Profile preview

ambrisentan + tadalafil

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

Overview

Ambrisentan + tadalafil is a fixed-dose combination of two oral small molecule drugs used to treat pulmonary arterial hypertension (PAH). Ambrisentan is an endothelin receptor antagonist that selectively blocks the type A endothelin receptor, preventing the action of endothelin-1, a potent vasoconstrictor, thereby relaxing blood vessels in the lungs and reducing blood pressure. Tadalafil is a phosphodiesterase-5 (PDE5) inhibitor that increases cyclic guanosine monophosphate (cGMP) levels in vascular smooth muscle by inhibiting its breakdown, leading to vasodilation and further reduction of pulmonary vascular resistance. The combination acts synergistically to improve hemodynamics and exercise capacity in patients with PAH by targeting complementary pathways involved in pulmonary vasoconstriction[1][4][5][6][8].

Other names
ambrisentan/tadalafil
02

Targets

EDNRA (Endothelin receptor type A)PDE5 (Phosphodiesterase 5A)

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