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Ambrisentan



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 search in 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

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

  1. ^ Vatter H, Seifert V (2006). "Ambrisentan, a non-peptide endothelin receptor antagonist". Cardiovasc Drug Rev 24 (1): 63-76. PMID 16939634.
  2. ^ Pollack, Andrew. "Gilead’s Drug Is Approved to Treat a Rare Disease", New York Times, 2007-06-16. Retrieved on 2007-05-25. 
  3. ^ 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.
  4. ^ 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.
  5. ^ Gilead Sciences (2007-03-23). "Marketing Authorisation Application for Ambrisentan Validated by European Medicines Agency". Press release. Retrieved on 2007-06-16.
  6. ^ 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 analoguesBeraprost, Epoprostenol, Iloprost, Treprostinil
Endothelin receptor antagonistsAmbrisentan, Bosentan, Sitaxsentan
PDE5 inhibitorsSildenafil, Tadalafil
Adjunctive therapyCalcium channel blockers, Diuretics, Digoxin, Oxygen therapy, Warfarin
v • d • e
Antihypertensives (C02) and diuretics (C03)
Sympatholytic agents (including alpha)centrally acting/antiadrenergics (Clonidine, Guanfacine, Methyldopa, Moxonidine, Rescinnamine, Reserpine, Rilmenidine) • ganglion-blocking/nicotinic antagonist (Mecamylamine, Trimethaphan) • peripherally acting/antiadrenergics (Prazosin, Guanethidine, Indoramin, Doxazosin)
VasodilatorsDiazoxide • Hydralazine • Minoxidil • Nitroprusside • Phentolamine
Other antihypertensivesserotonin antagonist (Ketanserin) • endothelin receptor antagonist (Bosentan, Ambrisentan, Sitaxsentan)
Low ceiling diureticsThiazide (Bendroflumethiazide, Chlorothiazide, Hydrochlorothiazide) • Chlortalidone • Indapamide • Quinethazone • Mersalyl • Metolazone • Theobromine • Cicletanine
High ceiling diureticsLoop diuretic (Bumetanide, Furosemide, Torasemide)
Potassium-sparing diureticsESC blockers (Amiloride, Triamterene) • aldosterone antagonists (Spironolactone, Eplerenone, Potassium canrenoate, Canrenone)
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Ambrisentan". A list of authors is available in Wikipedia.
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