| 词条 | Ambrisentan | ||||||
| 释义 |
| Watchedfields = changed | verifiedrevid = 437179007 | IUPAC_name = (2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid | image = Ambrisentan structure.svg | width = 200 | tradename = | Drugs.com = {{drugs.com|monograph|ambrisentan}} | licence_EU = yes | licence_US = Ambrisentan | pregnancy_AU = X | pregnancy_US = X | pregnancy_category = | legal_AU = S4 | legal_CA = Rx-only | legal_UK = POM | legal_US = Rx-only | legal_status = | routes_of_administration = Oral | bioavailability = Undetermined | protein_bound = 99% | metabolism = | elimination_half-life = 15 hours (terminal) | excretion = | IUPHAR_ligand = 3951 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 177036-94-1 | ATC_prefix = C02 | ATC_suffix = KX02 | PubChem = 6918493 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 5293690 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = HW6NV07QEC | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1111 | C=22 | H=22 | N=2 | O=4 | molecular_weight = 378.421 g/mol | smiles = O=C(O)[C@@H](Oc1nc(cc(n1)C)C)C(OC)(c2ccccc2)c3ccccc3 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = OUJTZYPIHDYQMC-LJQANCHMSA-N }} Ambrisentan (U.S. trade name Letairis; E.U. trade name Volibris; India trade name Pulmonext by MSN labs) is a drug indicated for use in the treatment of pulmonary hypertension. The peptide endothelin constricts muscles in blood vessels, increasing blood pressure. Ambrisentan, which relaxes those muscles, is an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA).[1] Ambrisentan significantly improved exercise capacity (6-minute walk distance) compared with placebo in two double-blind, multicenter trials (ARIES-1 and ARIES-2).[2] Ambrisentan was approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency, and designated an orphan drug, for the treatment of pulmonary hypertension.[3][4][5][6][7] Recent Developments and Publications
Clinical usesAmbrisentan 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. Birth defectsEndothelin receptor activation mediates strong pulmonary vasoconstriction and positive inotropic effect on the heart. These physiologic effects are vital for the development of the fetal cardiopulmonary system. In addition to this, endothelin receptors are also known to play a role in neural crest cell migration, growth, and differentiation. As such, endothelin receptor antagonists such as Ambrisentan are known to be teratogenic. Ambrisentan has a high risk of liver damage, and of birth defects if a woman becomes pregnant while taking it. In the U.S., doctors who prescribe it, and patients who take it, must enroll in a special program, the LETAIRIS Education and Access Program (LEAP), to learn about those risks. Ambrisentan is available only through specialty pharmacies. External links
References1. ^{{cite journal |author=Vatter H, Seifert V |title=Ambrisentan, a non-peptide endothelin receptor antagonist |journal=Cardiovasc Drug Rev |volume=24 |issue=1 |pages=63–76 |year=2006 |pmid=16939634 |doi=10.1111/j.1527-3466.2006.00063.x}} {{PAH rx}}{{Antihypertensives and diuretics}}{{Signaling peptide/protein receptor modulators}}{{Xenobiotic-sensing receptor modulators}}2. ^{{cite journal |vauthors=Frampton JE |title=Ambrisentan |journal=American Journal of Cardiovascular Drugs |volume=11 |issue=4 |pages=215–26 |year=2011 |pmid=21623643 |doi=10.2165/11207340-000000000-00000 }} 3. ^ {{cite news | last = Pollack | first = Andrew | title = Gilead’s Drug Is Approved to Treat a Rare Disease | work = The New York Times | date = 2007-06-16 | url = https://www.nytimes.com/2007/06/16/business/16gilead.html | accessdate = 2007-05-25| archiveurl= https://web.archive.org/web/20130524115948/http://www.nytimes.com/2007/06/16/business/16gilead.html| archivedate=May 24, 2013| deadurl= no}} 4. ^{{cite press release |title=U.S. Food and Drug Administration Approves Gilead's Letairis Treatment of Pulmonary Arterial Hypertension |publisher=Gilead Sciences |date=2007-06-15 |url=http://www.gilead.com/wt/sec/pr_1016053 |accessdate=2007-06-16 |deadurl=yes |archiveurl=https://web.archive.org/web/20070927064048/http://www.gilead.com/wt/sec/pr_1016053 |archivedate=2007-09-27 }} 5. ^{{cite press release | title = FDA Approves New Orphan Drug for Treatment of Pulmonary Arterial Hypertension | publisher = Food and Drug Administration | date = 2007-06-15 | url = http://www.fda.gov/bbs/topics/NEWS/2007/NEW01653.html | accessdate = 2007-06-22| archiveurl= https://web.archive.org/web/20070623055608/http://www.fda.gov/bbs/topics/NEWS/2007/NEW01653.html| archivedate= 23 June 2007 | deadurl= no}} 6. ^{{cite press release |title = GlaxoSmithKline's Volibris (ambrisentan) receives authorisation from the European Commission for the treatment of Functional Class II and III Pulmonary Arterial Hypertension |publisher = GlaxoSmithKline |date = 2008-04-25 |url = http://www.gsk.com/media/pressreleases/2008/2008_pressrelease_10033.htm |accessdate = 2008-04-29 |archiveurl = https://web.archive.org/web/20080430150346/http://www.gsk.com/media/pressreleases/2008/2008_pressrelease_10033.htm |archivedate = 2008-04-30 |deadurl = yes |df = }} 7. ^{{cite web | last = Waknine | first = Yael | title = International Approvals: Ambrisentan, Oral-lyn, Risperdal | publisher = Medscape | date = 2005-05-09 | url = http://www.medscape.com/viewarticle/504469 | accessdate = 2007-06-16}} 8. ^{{cite journal |vauthors=de Raaf MA, Beekhuijzen M, Guignabert C, Vonk Noordegraaf A, Bogaard HJ |title=Endothelin-1 receptor antagonists in fetal development and pulmonary arterial hypertension |journal=Reproductive Toxicology |volume=56 |issue= |pages=45–51 |year=2015 |pmid=26111581 |doi=10.1016/j.reprotox.2015.06.048 }} 9. ^{{cite journal |last1=Galiè |first1=Nazzareno |last2=Barberà |first2=Joan A. |last3=Frost |first3=Adaani E. |last4=Ghofrani |first4=Hossein-Ardeschir |last5=Hoeper |first5=Marius M. |last6=McLaughlin |first6=Vallerie V. |last7=Peacock |first7=Andrew J. |last8=Simonneau |first8=Gérald |last9=Vachiery |first9=Jean-Luc |last10=Grünig |first10=Ekkehard |last11=Oudiz |first11=Ronald J. |last12=Vonk-Noordegraaf |first12=Anton |last13=White |first13=R. James |last14=Blair |first14=Christiana |last15=Gillies |first15=Hunter |last16=Miller |first16=Karen L. |last17=Harris |first17=Julia H.N. |last18=Langley |first18=Jonathan |last19=Rubin |first19=Lewis J. |title=Initial Use of Ambrisentan plus Tadalafil in Pulmonary Arterial Hypertension |journal=New England Journal of Medicine |volume=373 |issue=9 |year=2015 |pages=834–44 |doi=10.1056/NEJMoa1413687 |pmid=26308684 }} 6 : Endothelin receptor antagonists|Ethers|Gilead Sciences|Orphan drugs|Pyrimidines|Carboxylic acids |
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