Ambrisentan
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| Ambrisentan
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| Systematic (IUPAC) name | |
| 2-(4,6-dimethylpyrimidin-2-yl)oxy-3-methoxy- 3,3-diphenyl-propanoic acid | |
| Identifiers | |
| CAS number | |
| ATC code | C02 |
| PubChem | |
| Chemical data | |
| Formula | C22H22N2O4 |
| Mol. mass | 378.421 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | Undetermined |
| Protein binding | 99% |
| Metabolism | ? |
| Half life | 15 hours (terminal) |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
X(US) May cause harm to fetus |
| Legal status | |
| Routes | Oral |
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]
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Overview
Ambrisentan (U.S. trade name Letairis) is a drug being researched for use in the treatment of pulmonary hypertension.
It functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA).[1]
Ambrisentan was approved for sale by the U.S. Food and Drug Administration (FDA) on June 15, 2007 for the once-daily treatment of pulmonary arterial hypertension.[2][3][4] The Marketing Authorisation Application is under review by the European Medicines Agency.[5] Ambrisentan had previously been designated an orphan drug by both the FDA and the European Commission, in August 2004 and May 2005 respectively.[6]
References
- ↑ Vatter H, Seifert V (2006). "Ambrisentan, a non-peptide endothelin receptor antagonist". Cardiovasc Drug Rev 24 (1): 63-76. PMID 16939634.
- ↑ Pollack, Andrew. "Gilead’s Drug Is Approved to Treat a Rare Disease", New York Times, 2007-06-16.
- ↑ Gilead Sciences (2007-06-15). U.S. Food and Drug Administration Approves Gilead's Letairis Treatment of Pulmonary Arterial Hypertension. Press release.
- ↑ Food and Drug Administration (2007-06-15). FDA Approves New Orphan Drug for Treatment of Pulmonary Arterial Hypertension. Press release.
- ↑ Gilead Sciences (2007-03-23). Marketing Authorisation Application for Ambrisentan Validated by European Medicines Agency. Press release.
- ↑ Waknine, Yael. International Approvals: Ambrisentan, Oral-lyn, Risperdal. Medscape.
Medications used in the management of pulmonary arterial hypertension (B01, C02) | |
|---|---|
| Prostacyclin analogues | Beraprost, Epoprostenol, Iloprost, Treprostinil |
| Endothelin receptor antagonists | Ambrisentan, Bosentan, Sitaxsentan |
| PDE5 inhibitors | Sildenafil, Tadalafil |
| Adjunctive therapy | Calcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin |
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