Zafirlukast

Zafirlukast

Clinical data
Pregnancy category	B1 (Au), B (U.S.)
Routes of administration	Oral
ATC code	R03DC01 (WHO)
Legal status
Legal status	POM (UK)
Pharmacokinetic data
Bioavailability	Unknown
Protein binding	99%
Metabolism	Hepatic (CYP2C9-mediated)
Elimination half-life	10 hours
Excretion	Biliary
Identifiers
IUPAC name cyclopentyl N-[3-{[2-methoxy-4-[(2-methylphenyl) sulfonylcarbamoyl]phenyl]methyl}-1-methyl-indol-5-yl] carbamate
CAS Number	107753-78-6
PubChem CID	5717
DrugBank	APRD00377
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C31H33N3O6S
Molar mass	575.676 g/mol

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

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.

External links

• Accolate, Accoleit, Vanticon (manufacturer's website)
• Zafirlukast (patient information)