Ambrisentan

Ambrisentan
(IUPAC) ime
(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy- 3,3-diphenylpropanoic acid
Klinički podaci
Identifikatori
CAS broj 177036-94-1
ATC kod C02KX02
PubChem[1][2] 6918493
ChemSpider[3] 5293690
ChEMBL[4] CHEMBL1111 DaY
Hemijski podaci
Formula C22H22N2O4 
Mol. masa 378.421 g/mol
SMILES eMolekuli & PubHem
Farmakokinetički podaci
Bioraspoloživost nepoznata
Vezivanje za proteine plazme 99%
Poluvreme eliminacije 15 časova
Farmakoinformacioni podaci
Licenca

EU EMEA:linkUS FDA:link

Trudnoća X(US)
Pravni status POM (UK) -only (SAD)
Način primene Oralno

Ambrisentan (USAN Letairis; E.U. trgovačko ime Volibris) je lek koji se koristi za lečenje pulmonarne hipertenzije.

On funkcioniše kao antagonist endotelinkog receptora, i selektivan je za tip A endotelinskog receptora (ETA).[5]

Ambrisentan je odobren za prodaju u SAD-u od strane FDA 15 juna 2007 kao jednodnevni tretman plućne hipertenzije.[6][7][8] Naknadno ga je odobrila Evropska Medicinska Agencija za upotrebu u EU aprila 2008.[9] Ambrisentan je označen kao orfanski lek od strane FDA i Evropske Komisije.[10]

Literatura

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  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. 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. 
  6. Pollack Andrew (2007). „Gilead’s Drug Is Approved to Treat a Rare Disease”. New York Times. Pristupljeno 2007. 
  7. "U.S. Food and Drug Administration Approves Gilead's Letairis Treatment of Pulmonary Arterial Hypertension" (Press release). Gilead Sciences. 2007. Archived from the original on 2007-09-27. Retrieved 2007. {{cite press release}}: Check date values in: |accessdate= (help); Unknown parameter |dead-url= ignored (|url-status= suggested) (help)
  8. "FDA Approves New Orphan Drug for Treatment of Pulmonary Arterial Hypertension" (Press release). Food and Drug Administration. 2007. Retrieved 2007. {{cite press release}}: Check date values in: |accessdate= (help)
  9. "GlaxoSmithKline's Volibris (ambrisentan) receives authorisation from the European Commission for the treatment of Functional Class II and III Pulmonary Arterial Hypertension" (Press release). GlaxoSmithKline. 2008. Archived from the original on 2008-04-30. Retrieved 2008. {{cite press release}}: Check date values in: |accessdate= (help); Unknown parameter |dead-url= ignored (|url-status= suggested) (help)
  10. Waknine Yael (2005). „International Approvals: Ambrisentan, Oral-lyn, Risperdal”. Medscape. Pristupljeno 2007. 

Spoljašnje veze

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