Drug intelligence / Profile preview

sildenafil + tadalafil + bosentan + macitentan

Development stage
Discontinued
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of four medications used in the treatment of pulmonary arterial hypertension (PAH): two phosphodiesterase-5 inhibitors (sildenafil and tadalafil) and two endothelin receptor antagonists (bosentan and macitentan). While these medications are commonly used in PAH treatment, this specific four-drug combination is not a standard therapeutic approach. In clinical practice, combinations typically involve one drug from each class rather than multiple drugs from the same class. The macitentan-tadalafil combination (OPSYNVI) has been approved as a single-tablet formulation, while bosentan-sildenafil combinations have been used but may have drug interaction concerns.

02

Targets

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

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