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20-September-2008 09:55:46 - Ambrisentan Ambrisentan Systematic IUPAC name 2-4,6-dimethylpyrimidin-2-yloxy-3-methoxy- 3,3-diphenyl-propanoic acid Identifiers CAS number 177036-94-1 ATC code C02KX02 PubChem 197712 Chemical data Formula C22H22N2O4 Mol. mass 378.421 g/mol SMILES eMolecules PubChem Pharmacokinetic data Bioavailability Undetermined Protein binding 99% Metabolism ? Half life 15 hours terminal Excretion ? Therapeutic considerations Licence data EU, US Pregnancy cat. XUS May cause harm to fetus Legal status POMUK ℞-onlyUS Routes Oral Ambrisentan U.S. trade name Letairis; E.U. tradename Volibris is a drug indicated 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.234 It was later approved by the European Medicines Agency for use in the EU on April 2008.5 Ambrisentan had previously been designated an orphan drug by both the FDA and the European Commission, in August 2004 and May 2005 respectively.6 Contents 1 Clinical uses 2 The LETAIRIS Education and Access Program 3 External links 4 References Clinical uses Ambrisentan is indicated for the treatment of pulmonary arterial hypertension WHO Group 1 in patients with WHO class II or III symptoms to improve exercise capacity and delay clinical worsening. The LETAIRIS Education and Access Program The LETAIRIS Education and Access Program LEAP is is a program to help physicians and patients learn about the risks of LETAIRIS, including the serious risks of liver injury and birth defects. LEAP works by: Providing information to prescribers on the risks of LETAIRIS Providing comprehensive education to patients and assistance with obtaining LETAIRIS Requiring enrollment of both prescriber and patient in LEAP Controlling dispensing through a specialized distribution network specialty pharmacies External links Letairis website run by Gilead Sciences Prescribing information Information on the LETAIRIS Education and Access Program LEAP References ^ Vatter H, Seifert V 2006. Ambrisentan, a non-peptide endothelin receptor antagonist. Cardiovasc Drug Rev 24 1: 63-76. doi:10.1111/j.1527-3466.2006.00063.x. PMID 16939634. ^ Pollack, Andrew 2007-06-16. Gilead's Drug Is Approved to Treat a Rare Disease, New York Times. Retrieved on 2007-05-25. ^ Gilead Sciences 2007-06-15. U.S. Food and Drug Administration Approves Gilead's Letairis Treatment of Pulmonary Arterial Hypertension. Press release. Retrieved on 2007-06-16. ^ Food and Drug Administration 2007-06-15. FDA Approves New Orphan Drug for Treatment of Pulmonary Arterial Hypertension. Press release. Retrieved on 2007-06-22. ^ GlaxoSmithKline 2008-04-25. GlaxoSmithKline's Volibris ambrisentan receives authorisation from the European Commission for the treatment of Functional Class II and III Pulmonary Arterial Hypertension. Press release. Retrieved on 2008-04-29. ^ Waknine, Yael 2005-05-09. International Approvals: Ambrisentan, Oral-lyn, Risperdal. Medscape. Retrieved on 2007-06-16. v d e 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 v d e Antihypertensives C02 and diuretics C03 Sympatholytic agents Centrally acting/antiadrenergics α2 agonist Clonidine, Guanfacine, Methyldopa imidazoline receptor agonist Moxonidine, Rilmenidine adrenergic uptake inhibitor Rescinnamine, Reserpine Ganglion-blocking/nicotinic antagonist Mecamylamine, Trimethaphan Peripherally acting/antiadrenergics α1 blockers: Prazosin Indoramin Trimazosin Doxazosin Urapidil Guanidine derivatives: Betanidine Guanethidine Guanoxan Debrisoquine Guanoclor Guanazodine Guanoxabenz Vasodilators Diazoxide hydrazinophthalazine Hydralazine, Dihydralazine, Endralazine, Cadralazine Minoxidil Nitroprusside Phentolamine Other antihypertensives serotonin antagonist Ketanserin endothelin receptor antagonist Bosentan, Ambrisentan, Sitaxsentan MAOI Pargyline THI Metirosine Diuretics Low ceiling Thiazides at DCT Bendroflumethiazide Hydroflumethiazide Hydrochlorothiazide Chlorothiazide Polythiazide Trichlormethiazide Cyclopenthiazide Methyclothiazide Cyclothiazide Mebutizide Sulfonamides Quinethazone Clopamide Chlortalidone Mefruside Clofenamide Metolazone Meticrane Xipamide Indapamide Clorexolone Fenquizone Other Mersalyl Theobromine Cicletanine osmotic Mannitol, Urea carbonic anhydrase inhibitor at PT Acetazolamide High ceiling Loop diuretic at AL Bumetanide, Furosemide, Torasemide, Ethacrynic acid Potassium-sparing at CD ESC blockers Amiloride, Triamterene aldosterone antagonists Spironolactone, Eplerenone, Potassium canrenoate, Canrenone Retrieved from http://en..org/wiki/Ambrisentan Categories: Endothelin receptor antagonists | Gilead Sciences | Orphan drugs Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch This page was last modified on 19 July 2008, at 00:19
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