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Sitaxentan information


Sitaxentan
Clinical data
Other namesTBC-11251
AHFS/Drugs.comInternational Drug Names
License data
  • EU EMA: by sitaxentan sodium
Routes of
administration		Oral
ATC code
  • C02KX03 (WHO)
Legal status
Legal status
  • Withdrawn
Pharmacokinetic data
Bioavailability70 to 100%
Protein binding>99%
MetabolismHepatic (CYP2C9- and CYP3A4-mediated)
Elimination half-life10 hours
ExcretionRenal (50 to 60%)
Fecal (40 to 50%)
Identifiers
IUPAC name
  • N-(4-chloro-3-methyl-5-isoxazolyl)-2-[[4,5-(methylenedioxy)-o-tolyl]acetyl]-3-thiophenesulfonamide
CAS Number
  • 184036-34-8
    210421-64-0 (sodium salt)
PubChem CID
  • 216235
IUPHAR/BPS
  • 3950
DrugBank
  • DB06268
ChemSpider
  • 21106381
UNII
  • J9QH779MEM
KEGG
  • D07171
ChEMBL
  • ChEMBL282724
CompTox Dashboard (EPA)
  • DTXSID0057673 Edit this at Wikidata
Chemical and physical data
FormulaC18H15ClN2O6S2
Molar mass454.90 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • Cc1cc2OCOc2cc1CC(=O)c3sccc3S(=O)(=O)Nc4onc(C)c4Cl

Sitaxentan sodium (TBC-11251) is a medication for the treatment of pulmonary arterial hypertension (PAH).[1] It was marketed as Thelin by Encysive Pharmaceuticals until Pfizer purchased Encysive in February 2008. In 2010, Pfizer voluntarily removed sitaxentan from the market due to concerns about liver toxicity.[2]

  1. ^ Barst RJ, Langleben D, Frost A, Horn EM, Oudiz R, Shapiro S, et al. (February 2004). "Sitaxsentan therapy for pulmonary arterial hypertension". American Journal of Respiratory and Critical Care Medicine. 169 (4): 441–447. doi:10.1164/rccm.200307-957OC. PMID 14630619.
  2. ^ Citing liver damage, Pfizer withdraws Thelin, Associated Press, December 12, 2010

and 11 Related for: Sitaxentan information

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Sitaxentan

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Sitaxentan sodium (TBC-11251) is a medication for the treatment of pulmonary arterial hypertension (PAH). It was marketed as Thelin by Encysive Pharmaceuticals...

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Endothelin receptor antagonist

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Three main kinds of ERAs exist: selective ETA receptor antagonists (sitaxentan, ambrisentan, atrasentan, BQ-123, sparsentan, zibotentan, avosentan, edonentan...

Word Count : 105

Sodium salts

Last Update:

Netobimin, ozagrel, pantoprazole, pemetrexed, secobarbital, sitamaquin, sitaxentan, sulfamiderazin, sulfapyridine, sulfaquinoxaline, sulfathiazole, sulfazecin...

Word Count : 314

Icos

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failure. Two drugs, sitaxentan sodium (also spelled sitaxsentan) and TBC3711, were tested in clinical trials under the partnership. Sitaxentan was designed to...

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ATC code C02

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Ketanserin C02KN01 Aprocitentan C02KX01 Bosentan C02KX02 Ambrisentan C02KX03 Sitaxentan C02KX04 Macitentan C02KX05 Riociguat C02KX52 Ambrisentan and tadalafil...

Word Count : 417

Thelin

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Thelin may refer to: Sitaxentan, a medication Björn Thelin (1942–2017), a member of The Spotnicks Eje Thelin (1938–1990), a Swedish trombonist Howard J...

Word Count : 105

Pulmonary hypertension

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is another ETA and ETB dual endothelin receptor blocker that is used. Sitaxentan (Thelin) was approved for use in Canada, Australia, and the European Union...

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List of withdrawn drugs

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Kingdom, and the United States Increased risk of heart attack and stroke. Sitaxentan 2010 Germany Hepatotoxicity. Sorivudine 1993 Japan Drug interaction and...

Word Count : 1956

Atrasentan

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antagonist selective for subtype A (ETA). While other drugs of this type (sitaxentan, ambrisentan) exploit the vasoconstrictive properties of endothelin and...

Word Count : 515

Endothelin

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hypertension, which was treatable in preliminary research by bosentan, sitaxentan or ambrisentan. Endothelins have involvement in cardiovascular function...

Word Count : 1655

Signaling peptide receptor

Last Update:

Darusentan Edonentan Enrasentan Fandosentan Feloprentan Macitentan Nebentan Sitaxentan Sparsentan Tezosentan Zibotentan Agonists Galanin Galanin (1-15) Galanin-like...

Word Count : 706
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