Active Ingredient History
Ambrisentan (alternative Names: BSF 208075; GSK 1325760; GSK1325760A; Letairis) is an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor. The chemical name of ambrisentan is (+)-(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid. Ambrisentan is indicated for the treatment of pulmonary arterial hypertension. It is approved in Europe, Canada and the United States for use as a single agent to improve exercise ability and delay clinical worsening. In addition, it is approved in the United States for use in combination with tadalafil to reduce the risks of disease progression, hospitalization and to improve exercise ability. As an endothelin receptor antagonist, ambrisentan prevents endogenous endothelin peptide from constricting the muscles in blood vessels, allowing them to relax and permit a reduction in blood pressure. Endothelin-1 (ET-1) is a potent autocrine and paracrine peptide. Two receptor subtypes, ETA and ETB, mediate the effects of ET-1 in the vascular smooth muscle and endothelium. The primary actions of ETA are vasoconstriction and cell proliferation, while the predominant actions of ETB are vasodilation, antiproliferation, and ET-1 clearance. In patients with PAH, plasma ET-1 concentrations are increased as much as 10-fold and correlate with increased mean right atrial pressure and disease severity. ET-1 and ET-1 mRNA concentrations are increased as much as 9-fold in the lung tissue of patients with PAH, primarily in the endothelium of pulmonary arteries. These findings suggest that ET-1 may play a critical role in the pathogenesis and progression of PAH. Ambrisentan is a high-affinity (Ki=0.011 nM) ETA receptor antagonist with a high selectivity for the ETA versus ETB receptor (>4000-fold). The clinical impact of high selectivity for ETA is not known. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Hypertension, Pulmonary (approved 2007)
Acute Kidney Injury (Phase 2)
Altitude Sickness (Phase 2/Phase 3)
Anemia, Sickle Cell (Phase 1)
Ascites (Phase 2)
Asthma (Phase 2)
Connective Tissue Diseases (Phase 4)
COVID-19 (Phase 2/Phase 3)
Dyspnea (Phase 4)
Fibrosis (Phase 2)
Healthy Volunteers (Phase 1)
Heart Diseases (Phase 2)
Heart Failure, Diastolic (Phase 4)
Heart Ventricles (Phase 4)
Hypertension ()
Hypertension, Portal (Phase 2)
Hypertension, Pulmonary (Phase 4)
Hypoplastic Left Heart Syndrome (Phase 2)
Hypoxia (Phase 2)
Idiopathic Pulmonary Fibrosis (Phase 3)
Liver Cirrhosis (Phase 4)
Pulmonary Arterial Hypertension (Phase 4)
Sarcoidosis (Phase 2/Phase 3)
Scleroderma, Systemic (Phase 4)
Vascular Diseases (Phase 3)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
Feedback
Data collection and curation is an ongoing process for CDEK - if you notice any information here to be missing or incorrect, please let us know! When possible, please include a source URL (we verify all data prior to inclusion).
Report issue
