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ambrisentan + tadalafil + treprostinil
- Development stage
- Unknown
- Lead developer
- Gilead Sciences
- Modality
- Small Molecules
- Administration
- Oral, Subcutaneous
01
Overview
A triple combination therapy used for treating severe pulmonary arterial hypertension (PAH). This combination targets multiple pathways involved in PAH pathophysiology: ambrisentan blocks endothelin receptor type A, tadalafil inhibits phosphodiesterase type 5, and treprostinil acts as a prostacyclin analogue promoting vasodilation and inhibiting platelet aggregation. Clinical studies have shown significant improvements in hemodynamics, right ventricular structure and function, and functional status in patients with severe PAH.
02
Targets
PTGIR (Prostanoid IP Receptor)PPARD (Peroxisome proliferator–activated receptor delta)EDNRA (Endothelin receptor type A)PDE5 (Phosphodiesterase 5A)PTGER2 (Prostaglandin E2 receptor EP2)EDNRB (Endothelin receptor type B)PTGDR (Prostanoid DP1 receptor)
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