Details of the Drug Formulation (DFM)

General Information of DFM (ID: F03953)
Name
Cetirizine 5 mg tablet
Company
Sandoz
Active Pharmaceutical Ingredient (API) Cetirizine API Info click to show the detail info of this API
Allergy ICD-11: 4A80 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0TU6R DIG Info Acesulfame Flavoring agent
E0NY1O DIG Info Benzyl alcohol Antimicrobial preservative ...
E0NN4I DIG Info Dextrin Binding agent ...
E09YYN DIG Info Eisenoxyd Colorant
E0M0IE DIG Info Ferric hydroxide oxide yellow Colorant
E00DHW DIG Info Lactose monohydrate Binding agent ...
E01UTP DIG Info Magnesium stearate lubricant
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0QY1F DIG Info Talc Anticaking agent ...
E09WWS DIG Info Tocopheryl acetate Antioxidant
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            DBT Name: Indoleamine 2,3-dioxygenase 1 (IDO1) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Benzyl alcohol
                    Biological Activity IC50 = 1400 nM (estimated based on the structural similarity with CHEMBL3763371 ) [1]
                    Structural Similarity Tanimoto coefficient = 0.848101266
                    Tested Species Homo sapiens (Human)
                    UniProt ID I23O1_HUMAN
            DBT Name: Albendazole monooxygenase (CYP3A4) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Propylene glycol
                    Biological Activity Inhibition ratio < 20 % (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase II (CA2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Acesulfame
                    Biological Activity Ki > 20000 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
            DBT Name: Carbonic anhydrase IX (CA9) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Acesulfame
                    Biological Activity Ki = 2400 nM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH9_HUMAN
      Cell line (CELL)
            DBT Name: Colon cancer Caco-2 cells (Caco-2) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Dextrin
                    Biological Activity Inhibition ratio > 55 % (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
            DBT Name: Prostate cancer LNCaP cells (LNCaP) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocopheryl acetate
                    Biological Activity EC50 = 38000 nM (estimated based on the structural similarity with CHEMBL242495 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.933333333
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0395
            DBT Name: Breast cancer MCF7 cells (MCF7) Click to Show/Hide
               Detailed Information DBT Info click to show the detail info of this DBT
               Experiment for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocopheryl acetate
                    Biological Activity IC50 > 500000 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0031
References
1 O-alkylhydroxylamines as rationally-designed mechanism-based inhibitors of indoleamine 2,3-dioxygenase-1. Eur J Med Chem. 2016 Jan 27; 108:564-576.
2 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
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 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.
5 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.
6 First pharmacophore-based identification of androgen receptor down-regulating agents: discovery of potent anti-prostate cancer agents. Bioorg Med Chem. 2007 May 15; 15(10):3413-21.
7 Design and synthesis of analogs of vitamin E: antiproliferative activity against human breast adenocarcinoma cells. Bioorg Med Chem Lett. 1998 Sep 22; 8(18):2433-8.

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