Article: Zafirlukast

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Zafirlukast
Systematic (IUPAC) name
cyclopentyl N-[3-{[2-methoxy-4-[(2-methylphenyl)
sulfonylcarbamoyl]phenyl]methyl}-1-methyl-indol-5-yl] carbamate
Identifiers
CAS number 107753-78-6
ATC code R03DC01
PubChem 5717
DrugBank APRD00377
Chemical data
Formula C31H33N3O6S 
Mol. weight 575.676 g/mol
Pharmacokinetic data
Bioavailability Unknown
Protein binding 99%
Metabolism Hepatic (CYP2C9-mediated)
Half life 10 hours
Excretion Biliary
Therapeutic considerations
Pregnancy cat.

B1 (Au), B (U.S.)

Legal status

POM (UK)

Routes Oral

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma. It is available as a tablet.

Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.

Zafirlukast is marketed by AstraZeneca with the brand names Accolate, Accoleit, and Vanticon. It was the first LTRA to be marketed in the USA and is now approved in over 60 countries, including the UK, Japan, Italy, Spain, Canada, Brazil and China.


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