Details of the Drug Formulation (DFM)

General Information of DFM (ID: F23576)
Name
Tolmetin Sodium eq 400mg base capsule
Company
Ortho Mcneil Janssen
Active Pharmaceutical Ingredient (API) Tolmetin API Info click to show the detail info of this API
Rheumatoid arthritis ICD-11: FA20 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E05PRI DIG Info Erythrosine sodium anhydrous Colorant
E00FTX DIG Info Gelatin Other agent
E01UTP DIG Info Magnesium stearate lubricant
E0ST5E DIG Info Pregelatinized starch Binding agent ...
E0L0MR DIG Info Sunset yellow FCF Colorant
E0QY1F DIG Info Talc Anticaking agent ...
E05BSD DIG Info Titanium dioxide Coating agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            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 Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    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 Pregelatinized starch
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    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 Pregelatinized starch
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
            DBT Name: Cytochrome P450 2E1 (CYP2E1) 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 Gelatin
                    Biological Activity IC50 = 141.2 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Cytochrome P450 2C9 (CYP2C9) 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 Gelatin
                    Biological Activity EC50 = 249.5 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
            DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) 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 Gelatin
                    Biological Activity EC50 = 20.5 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2CJ_HUMAN
            DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) 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 Gelatin
                    Biological Activity EC50 = 379.9 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2D6_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Cholesterol 25-hydroxylase (CYP1A2) 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 Gelatin
                    Biological Activity IC50 = 40.9 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      Primary active transporter (PAT)
            DBT Name: Multidrug resistance protein 3 (ABCC3) 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 Erythrosine sodium anhydrous
                    Biological Activity IC50 = 133000 nM (estimated based on the structural similarity with CHEMBL177756 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.90070922
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP3_HUMAN
            DBT Name: Multidrug resistance protein 4 (ABCC4) 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 Erythrosine sodium anhydrous
                    Biological Activity IC50 = 133000 nM (estimated based on the structural similarity with CHEMBL177756 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.90070922
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP4_HUMAN
            DBT Name: Multidrug resistance protein 1 (ABCB1) 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 Pregelatinized starch
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO2B1 (OATPB) 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 Sunset yellow FCF
                    Biological Activity Inhibition ratio = 54.5 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sunset yellow FCF
                    Biological Activity Ki = 68.4 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sunset yellow FCF
                    Biological Activity Ki = 74 uM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Other protein families (OPF)
            DBT Name: Thrombopoietin receptor (MPL) 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 Sunset yellow FCF
                    Biological Activity EC50 = 3000 nM (estimated based on the structural similarity with CHEMBL122867 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.93081761
                    Tested Species Homo sapiens (Human)
                    UniProt ID TPOR_HUMAN
References
1 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
2 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov; 136(1):216-41.
4 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
5 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
6 Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis. J Med Chem. 2001 Oct 25; 44(22):3730-45.

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