-5%
Embelin is used for the treatment of Pulmonary Arterial Hypertension (PAH) (WHO Group 1) to improve exercise capacity and delay clinical deterioration.
- Use as per the guidance of a registered healthcare professional.
Endothelin-1 (ET-1) is a powerful peptide involved in various vascular actions. It exerts its effects through two receptor subtypes: ETA and ETB. ETA primarily causes vasoconstriction and cell proliferation, while ETB induces vasodilation, antiproliferation, and ET-1 clearance. Ambrisentan is a potent ETA receptor antagonist, with over 4000 times greater selectivity for ETA over ETB. The exact clinical significance of this high selectivity is not well understood.
Ambrisentan is absorbed with peak levels appearing about 2 hours after oral administration, and food does not affect its absorption. It is highly bound to plasma proteins (99%) and eliminated through non-renal pathways. Although its terminal half-life is around 15 hours, the accumulation factor after long-term dosing indicates an effective half-life of about 9 hours.