Ambrisentan

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Ambrisentan
Systematic (IUPAC) name
2-(4,6-dimethylpyrimidin-2-yl)oxy-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
Pregnancy cat.	X(US) May cause harm to fetus
Legal status	℞-only(US)
Routes	Oral

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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 (ET_A).^[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.^[1][1][1] The Marketing Authorisation Application is under review by the European Medicines Agency.^[1] Ambrisentan had previously been designated an orphan drug by both the FDA and the European Commission, in August 2004 and May 2005 respectively.^[1]

References

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 Alpha 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 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 High ceiling Loop diuretic (Bumetanide, Furosemide, Torsemide) Potassium-sparing ESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .