Drug intelligence / Profile preview

bosentan + tadalafil

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Combination of **bosentan**, an endothelin receptor antagonist (ERA), and **tadalafil**, a phosphodiesterase type 5 (PDE5) inhibitor. Both are oral small molecule drugs approved as monotherapy for treatment of **pulmonary arterial hypertension** (PAH). Bosentan blocks endothelin-1 from activating endothelin A and B receptors, resulting in vasodilation and antiproliferative effects. Tadalafil inhibits PDE5, increasing cGMP levels and causing relaxation of pulmonary vascular smooth muscle. This specific combination (bosentan + tadalafil) is studied as combination therapy in PAH to potentially enhance hemodynamic and clinical benefit via complementary pathways.

02

Targets

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

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