Sitaksentan
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| |||
| (IUPAC) ime | |||
|---|---|---|---|
| N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-2H-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide | |||
| Klinički podaci | |||
| Identifikatori | |||
| CAS broj | 184036-34-8 210421-64-0 (natrijumska so) | ||
| ATC kod | C02KX03 | ||
| PubChem[1][2] | 216235 | ||
| ChemSpider[3] | 21106381 | ||
| Hemijski podaci | |||
| Formula | C18H15ClN2O6S2 | ||
| Mol. masa | 454.906 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
| |||
| Sinonimi | Sitaksentan; TBC-11251 | ||
| Farmakokinetički podaci | |||
| Bioraspoloživost | 70 to 100% | ||
| Vezivanje za proteine plazme | >99% | ||
| Metabolizam | Hepatički (CYP2C9- i CYP3A4-posredovano) | ||
| Poluvreme eliminacije | 10 sati | ||
| Izlučivanje | Renalno (50 do 60%) Fekalno (40 do 50%) | ||
| Farmakoinformacioni podaci | |||
| Licenca | |||
| Trudnoća | ? | ||
| Pravni status | Samo na recept (S4) (AU) POM (UK) | ||
| Način primene | Oralno | ||
Sitaksentan natrijum (TBC-11251) je lek za tretman plućne hipertenzije.[4] On je bio u prodaji pod imenom Telin od strane Encisive Farmaceutikals, sve dok Pfizer nije kupio tu kompaniju februara 2008. Pfizer je dobrovoljno povukao sitaksentan sa tržišta 2010. godine zbog moguće toksičnosti jetre.[5]
Mehanizam dejstva[uredi | uredi kod]
Sitaksentan je mali molekul koji selektivno blokira dejstvo endotelina na endotelinskom-A (ETA) receptoru (oko 6000 puta je potentniji u odnosu na ETB).[6] On pripada sulfonamidnoj klasi antagonista endotelinkog receptora.
Reference[uredi | uredi kod]
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Barst RJ, Langleben D, Frost A et al. (2004). „Sitaxsentan therapy for pulmonary arterial hypertension”. American Journal of Respiratory Critical Care Medicine 169 (4): 441–447. DOI:10.1164/rccm.200307-957OC.
- ↑ „Citing liver damage, Pfizer withdraws Thelin, Associated Press, December 12, 2010”. Arhivirano iz originala na datum 2010-12-13. Pristupljeno 2014-04-05.
- ↑ Girgis, RE; Frost, AE; Hill, NS; Horn, EM; Langleben, D; McLaughlin, VV; Oudiz, RJ; Robbins, IM i dr.. (2007). „Selective endothelin A receptor antagonism with sitaxsentan for pulmonary arterial hypertension associated with connective tissue disease.”. Annals of the rheumatic diseases 66 (11): 1467–72. DOI:10.1136/ard.2007.069609. PMC 2111639. PMID 17472992.
Literatura[uredi | uredi kod]
- Mucke HAM (2009). „Sitaxsentan for the Oral Treatment of Pulmonary Arterial Hypertension: Benefits from Endothelin Receptor Subtype Selectivity?”. Clinical Medicine: Therapeutics 1: 111–121.
- Robyn J. Barst, MD; Stuart Rich, MD, FCCP; Allison Widlitz, MS, PA; Evelyn M. Horn, MD; Vallerie McLaughlin, MD and Joyce McFarlin, RN (2002). „1860-1868”. Arhivirano iz originala na datum 2003-08-04. Pristupljeno 2014-04-05.
