Substance
ID:4559
Names and Identifiers
Synonyms
TBC-11251SitaxsentanSitaxentan
Brand Name
Thelin
IUPAC name
N-(4-chloro-3-methyl-1,2-oxazol-5-yl)-2-[2-(6-methyl-2H-1,3-benzodioxol-5-yl)acetyl]thiophene-3-sulfonamide
IUPAC Traditional name
sitaxentan
Properties
No Data Available
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Molecule Details
Drug Groups
approved; investigational
Indication
Investigated for use/treatment in pulmonary hypertension, connective tissue diseases, hypertension, and congestive heart failure.
Pharmacology
Sitaxentan belongs to a class of drugs known as endothelin receptor antagonists (ERAs). Patients with PAH have elevated levels of endothelin, a potent blood vessel constrictor, in their plasma and lung tissue. Sitaxentan blocks the binding of endothelin to its receptors, thereby negating endothelin's deleterious effects.
Biotransformation
Hepatic (CYP2C9- and CYP3A4-mediated)
Absorption
70-100%
Half Life
10 hours
Protein Binding
99% +
Elimination
Renal (50 to 60%)
Fecal (40 to 50%)
Fecal (40 to 50%)
External Links
Molecular Spectra
No Data Available
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References
No Data Available
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