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:link, US 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

  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. 

Vanjske veze

Portal Medicina
Portal Hemija