Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00737)
Name
Zafirlukast
Synonyms    Click to Show/Hide the Synonyms of This API
zafirlukast; 107753-78-6; Accolate; Olmoran; ICI-204219; Accoleit; ICI 204219; ICI 204,219; C31H33N3O6S; UNII-XZ629S5L50; Zafirlukast (Accolate); CHEMBL603; Aeronix; CHEBI:10100; XZ629S5L50; MFCD00864775; NCGC00164547-01; NCGC00164547-06; Vanticon; DSSTox_CID_3746; DSSTox_RID_77181; DSSTox_GSID_23746; Zafirst; Respix; Accolate (TN); SMR000466316; CAS-107753-78-6; SR-01000759386; Zafirlucast; Zafirlukast (JAN/USAN/INN); Zafirlukast [USAN:INN:BAN]; Zafirlukast(Accolate); PubChem18223; CPD000466316; ACMC-209wlw; SCHEMBL4175; MLS000759421; MLS001424064; MLS006011771; BIDD:GT0267; GTPL3322; DTXSID5023746; Zafirlukast, >=98% (HPLC); HMS2051F12; HMS2089J10; HMS3393F12; HMS3650A04; HMS3655E13; HMS3713J08; HMS3745K03; ZINC896717; BCP05226; Tox21_112176; ANW-46530; BDBM50009073; STK646780; AKOS005577888; Tox21_112176_1; AC-9018; CCG-101025; DB00549; MCULE-2053856450; NC00275; SB19079; NCGC00164547-02; NCGC00164547-03; NCGC00164547-04; NCGC00164547-05; AS-12943; BR-72849; HY-17492; AB0012638; FT-0601575; MLS000759421-02; SW197655-3; C07206; D00411; 32256-EP2270008A1; 32256-EP2280006A1; 32256-EP2281813A1; 32256-EP2281815A1; 32256-EP2281819A1; 32256-EP2284166A1; 32256-EP2292617A1; 32256-EP2292619A1; 32256-EP2295409A1; 32256-EP2298415A1; 32256-EP2301933A1; 32256-EP2305640A2; 32256-EP2305659A1; 32256-EP2308562A2; 32256-EP2311818A1; 32256-EP2311827A1; AB00639922-06; AB00639922-08; AB00639922_09; 753Z786; A801752; L001011; Q928378; Q-201940; SR-01000759386-4; SR-01000759386-5; SR-01000759386-9; BRD-K71289571-001-06-4; Z1551429730
Clinical Status
Approved
Disease Indication Asthma ICD-11: CA23 [1]
PubChem CID
5717
Formula
C31H33N3O6S
Canonical SMILES
CC1=CC=CC=C1S(=O)(=O)NC(=O)C2=CC(=C(C=C2)CC3=CN(C4=C3C=C(C=C4)NC(=O)OC5CCCC5)C)OC
InChI
1S/C31H33N3O6S/c1-20-8-4-7-11-29(20)41(37,38)33-30(35)22-13-12-21(28(17-22)39-3)16-23-19-34(2)27-15-14-24(18-26(23)27)32-31(36)40-25-9-5-6-10-25/h4,7-8,11-15,17-19,25H,5-6,9-10,16H2,1-3H3,(H,32,36)(H,33,35)
InChIKey
YEEZWCHGZNKEEK-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=5717"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 575.7 Topological Polar Surface Area 124
XlogP 5.5 Complexity 1010
Heavy Atom Count 41 Rotatable Bond Count 9
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Zafirlukast 20 mg tablet Click to Show/Hide the Full List of Formulation(s):          9 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Hypromellose; Povidone
                   Dosage Form Oral Tablet
                   Company State of Florida DOH Central Pharmacy
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Povidone; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company AstraZeneca; Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose, unspecified form; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company Avera McKennan Hospital; Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Dr Reddy's Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
             Drug Formulation 7 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Carilion Materials Management
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
             Drug Formulation 8 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
             Drug Formulation 9 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose (1200000 mw); Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company AvPAK
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
          Zafirlukast 10 mg tablet Click to Show/Hide the Full List of Formulation(s):          5 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Povidone; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company AstraZeneca; Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose, unspecified form; Magnesium stearate; Titanium dioxide; Croscarmellose sodium; Cellulose, microcrystalline; Hypromelloses; Povidones
                   Dosage Form Oral Tablet
                   Company Par Pharmaceutical
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [3]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Titanium dioxide; Polyethylene glycol 400; Cellulose, microcrystalline; Hydroxypropyl cellulose; Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Dr Reddy's Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [3]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [4]
References
1 FDA label for approved zafirlukast from the official website of the U.S. Food and Drug Administration.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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