Active Ingredient History

NOW
  • Now
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. Zafirlukast is indicated for the prophylaxis and chronic treatment of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD4 than nonasthmatic subjects. In vitro studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC4, LTD4 and LTE4) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD4-induced increases in cutaneous vascular permeability and inhibited inhaled LTD4-induced influx of eosinophils into animal lungs. Zafirlukast is a selective and competitive receptor antagonist of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. Zafirlukast is marketed by Astra Zeneca 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, Taiwan, Italy, Spain, Canada, Brazil, China and Turkey.   NCATS

  • SMILES: COC1=CC(=CC=C1CC2=CN(C)C3=C2C=C(NC(=O)OC4CCCC4)C=C3)C(=O)NS(=O)(=O)C5=CC=CC=C5C
  • InChIKey: YEEZWCHGZNKEEK-UHFFFAOYSA-N
  • Mol. Mass: 575.675
  • ALogP: 5.7
  • ChEMBL Molecule:
More Chemistry
  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$0.3960 - $3.7358
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

4-(5-cyclopentyloxycarbonylamino-1-methyl-1h-indol-3-ylmethyl)-3-methoxy-n-o-tolylsulfonylbenzamide | 4-(5-cyclopentyloxycarbonylamino-2-methylindol-3-yl-methyl)-3-methoxy-n-o-tolylsulfonylbenzamide | accolate | aeronix | cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate | ici 204219 | ici 204,219 | ici-204219 | ici-204,219 | olmoran | vanticon | zafirlukast

Feedback

Data collection and curation is an ongoing process for CDEK - if you notice any information here to be missing or incorrect, please let us know! When possible, please include a source URL (we verify all data prior to inclusion).

Report issue