Details of the Drug Formulation (DFM)

General Information of DFM (ID: F18897)
Name
Repaglinide 0.5 mg tablet
Company
Paddock Laboratories,
Active Pharmaceutical Ingredient (API) Repaglinide API Info click to show the detail info of this API
Diabetes mellitus ICD-11: 5A10 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0Q8ZK DIG Info Calcium hydrogenphosphate Diluent
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E01UTP DIG Info Magnesium stearate lubricant
E0DS2Q DIG Info Meglumine Buffering agent
E0E7MW DIG Info Poloxamer 407 Emulsifying agent ...
E01UTV DIG Info Silicon dioxide Anticaking 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 Calcium hydrogenphosphate
                    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 Poloxamer 407
                    Biological Activity EC50 = 32.8 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Silicon dioxide
                    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 Poloxamer 407
                    Biological Activity IC50 = 218.9 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 Poloxamer 407
                    Biological Activity EC50 = 355 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_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 Poloxamer 407
                    Biological Activity EC50 = 101.6 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2D6_HUMAN
      Transferase (TFase)
            DBT Name: Alglucerase (GBA) 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 Meglumine
                    Biological Activity IC50 = 447000 nM (estimated based on the structural similarity with CHEMBL1933095 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.846153846
                    Tested Species Bos taurus (Bovine)
                    UniProt ID GLCM_BOVIN
      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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Poloxamer 407
                    Biological Activity Inhibition ratio = 38 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Poloxamer 407
                    Biological Activity Inhibition ratio > 45 % (tested by experiment) [5]
                    Tested Species Homo sapiens (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 Towards a stable noeuromycin analog with a D-manno configuration: synthesis and glycosidase inhibition of D-manno-like tri- and tetrahydroxylated azepanes. Bioorg Med Chem. 2012 Jan 15; 20(2):641-9.
4 Inhibition of human efflux transporter ABCC2 (MRP2) by self-emulsifying drug delivery system: influences of concentration and combination of excipients. J Pharm Pharm Sci. 2014;17(4):447-60.
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.

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