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Systematic (IUPAC) name
cyclopentyl N-[3-{[2-methoxy-4-[(2-methylphenyl)
sulfonylcarbamoyl]phenyl]methyl}-1-methyl-indol-5-yl] carbamate
CAS number 107753-78-6
ATC code R03DC01
PubChem 5717
DrugBank APRD00377
Chemical data
Formula C31H33N3O6S 
Mol. mass 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


Routes Oral

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), which is usually taken just once daily.

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, China and Turkey.

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Zafirlukast". A list of authors is available in Wikipedia.
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