Drug intelligence / Profile preview

bosentan + sildenafil

Development stage
Phase 4
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral
01

Overview

Bosentan + sildenafil is a combination therapy consisting of two small molecule drugs used primarily for the treatment of pulmonary arterial hypertension (PAH) and severe pulmonary hypertension. Bosentan is an endothelin receptor antagonist that blocks the action of endothelin-1, a potent vasoconstrictor, on the endothelin A and B receptors in vascular smooth muscle, leading to vasodilation and reduced blood pressure in the pulmonary arteries. Sildenafil is a phosphodiesterase type 5 (PDE5) inhibitor that increases cyclic guanosine monophosphate (cGMP) levels by inhibiting its breakdown, resulting in relaxation of vascular smooth muscle and further vasodilation. The combination aims to improve cardiac function, exercise capacity, and symptoms in patients with PAH or related conditions. Clinical studies have shown that this combination can be effective but may also result in significant drug-drug interactions affecting plasma concentrations of both agents[1][2][3][4][5].

Other names
Bosentan and Sildenafil combination therapySildenafil/Bosentan
02

Targets

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

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