Repositioning Candidate Details
| Candidate ID: | R0187 |
| Source ID: | DB00549 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Zafirlukast |
| Synonyms: | 4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate; Zafirlukast |
| Molecular Formula: | C31H33N3O6S |
| SMILES: | COC1=CC(=CC=C1CC1=CN(C)C2=C1C=C(NC(=O)OC1CCCC1)C=C2)C(=O)NS(=O)(=O)C1=CC=CC=C1C |
| Structure: |
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| DrugBank Description: | 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. |
| CAS Number: | 107753-78-6 |
| Molecular Weight: | 575.675 |
| DrugBank Indication: | For the prophylaxis and chronic treatment of asthma. |
| DrugBank Pharmacology: | Zafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) 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 LTD<sub>4</sub> than nonasthmatic subjects. <i>In vitro</i> studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC<sub>4</sub>, LTD<sub>4</sub> and LTE<sub>4</sub>) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD<sub>4</sub>-induced increases in cutaneous vascular permeability and inhibited inhaled LTD<sub>4</sub>-induced influx of eosinophils into animal lungs. |
| DrugBank MoA: | Zafirlukast is a selective and competitive receptor antagonist of leukotriene D4 and E4 (LTD<sub>4</sub> 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. |
| Targets: | Cysteinyl leukotriene receptor 1 antagonist |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Diseases ID | DO ID | Disease Name | Definition | Class |
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