Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00360)
Name
Levocetirizine
Synonyms    Click to Show/Hide the Synonyms of This API
Levocetirizine; 130018-77-8; (R)-cetirizine; Levocetirizine HCl; (-)-Cetirizine; UNII-6U5EA9RT2O; (R)-2-(2-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethoxy)acetic acid; (R)-Cetirizine dihydrochloride; 6U5EA9RT2O; Xarlin; Acetic acid, (2-(4-((R)-(4-chlorophenyl)phenylmethyl)-1-piperazinyl)ethoxy)-; (2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid; 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]piperazin-1-ium-1-yl]ethoxy]acetate; SMR000466315; R-levocetirizine; Levocetirizine [USAN:INN:BAN]; Cetirizine (r)-form; Xazal (TN); PubChem21319; Cetirizine (-) isomer; SCHEMBL4914; Levocetirizine (USAN/INN); MLS000759420; MLS001401375; BIDD:GT0791; Singulair and xyzal combination; GTPL1214; CHEMBL1201191; BDBM85030; CHEBI:94559; DTXSID60156294; HCP1102; 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic acid; HMS2051N10; HMS2231M24; HCP 1102; HY-B0814; CL0022; PDSP1_000117; PDSP1_000269; PDSP2_000117; PDSP2_000268; ZINC19364230; (2-(4-((R-p-Chloro-alpha-phenylbenzyl)-1-piperazinyl)ethoxy)acetic acid; AKOS016844241; CCG-101021; DB06282; NCGC00263567-04; AC-15295; CS-0012812; 18L778; D07402; AB00639972-08; Q421091; H230000000; UNII-YO7261ME24 component ZKLPARSLTMPFCP-OAQYLSRUSA-N; 2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
Clinical Status
Approved
Disease Indication Allergic rhinitis ICD-11: CA08 [1]
PubChem CID
1549000
Formula
C21H25ClN2O3
Canonical SMILES
C1CN(CCN1CCOCC(=O)O)[C@H](C2=CC=CC=C2)C3=CC=C(C=C3)Cl
InChI
1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26)/t21-/m1/s1
InChIKey
ZKLPARSLTMPFCP-OAQYLSRUSA-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=1549000"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 388.9 Topological Polar Surface Area 53
XlogP 1.7 Complexity 443
Heavy Atom Count 27 Rotatable Bond Count 8
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 5
Full List of Drug Formulations (DFMs) Containing This API
          Levocetirizine 5 mg tablet Click to Show/Hide the Full List of Formulation(s):        19 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; Polyethylene glycol 400; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Macleods Pharmaceuticals
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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
Anhydrous lactose; Magnesium stearate; Titanium dioxide; Polysorbate 80; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Aidarex Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Polyethylene glycol 400; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company ScieGen Pharmaceuticals; Vensun Pharmaceuticals
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Polyethylene glycol 400; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s)
                   Dosage Form Oral Tablet
                   Company Micro Labs
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s)
                   Dosage Form Oral Tablet
                   Company Dispensing Solution; Lake Eire Medical & Surgical Supply DBA Quality Care Products; PD-Rx Pharmaceuticals
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Silicon dioxide; Hypromellose 2910 (5 mpa.s); Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Teva Pharmaceuticals
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Ranbaxy Pharmaceuticals
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Polysorbate 80; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company American Health Packaging; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             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; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company AvKARE; Yiling 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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 10 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; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Carlsbad Technology; Proficient Rx
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 11 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; Silicon dioxide; Hypromellose, unspecified; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack; Glenmark Pharmaceutials
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 12 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; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols
                   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) [2]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 13 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; Polysorbate 80; Cellulose, microcrystalline; Colloidal silicon dioxide; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 14 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; Polysorbate 80; Cellulose, microcrystalline; Colloidal silicon dioxide; Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Camber Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polysorbate 80 DIG Info Prostaglandin G/H synthase 1 (IC50 = 1 uM) [4]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 15 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; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycols
                   Dosage Form Oral Tablet
                   Company Apotex; Preferred Pharamaceuticals
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
             Drug Formulation 16 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; Hydroxypropyl cellulose (1200000 mw); Hypromellose, unspecified; Microcrystalline cellulose; Polyethylene glycol, unspecified
                   Dosage Form Oral Tablet
                   Company Proficient Rx
                   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) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
             Drug Formulation 17 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; Hypromelloses; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Chattem
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
             Drug Formulation 18 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; Hypromellose; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   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) [5]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
             Drug Formulation 19 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; Hypromelloses
                   Dosage Form Oral Tablet
                   Company Perrigo New York; Physicians Total Care
                   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) [2]
Polyethylene glycol 400 DIG Info Albendazole monooxygenase (IC50 = 10.77 mg.mL-1) [3]
References
1 FDA label for approved levocetirizine from the official website of the U.S. Food and Drug Administration.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
4 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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