Article: Zafirlukast

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.