Details of the Drug Formulation (DFM)

General Information of DFM (ID: F07937)
Name
Felodipine 5 mg tablet
Company
Wockhardt
Active Pharmaceutical Ingredient (API) Felodipine API Info click to show the detail info of this API
Essential hypertension ICD-11: BA00 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0VK1L DIG Info Hydrogenated polyoxyl 40 castor oil Emulsifying agent ...
E00DHW DIG Info Lactose monohydrate Binding agent ...
E0H6BT DIG Info Quinoline yellow WS Colorant
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0RS6F DIG Info Sodium stearyl fumarate lubricant
E0L0MR DIG Info Sunset yellow FCF Colorant
E05BSD DIG Info Titanium dioxide Coating agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Alpha-2A adrenoceptor (ADA2A) 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 Quinoline yellow WS
                    Biological Activity IC50 = 28 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA2A_HUMAN
            DBT Name: Dopamine D3 receptor (DRD3) 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 Quinoline yellow WS
                    Biological Activity IC50 = 26 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD3_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Cytochrome P450 3A (CYP3A) 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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity Protein expression downregulation (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 800 uM (tested by experiment) [3]
                    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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 0.25 mg.mL-1 (tested by experiment) [4]
                    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) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 30 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
      Hydrolase (HDase)
            DBT Name: Acetylcholinesterase (ACHE) 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 Quinoline yellow WS
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACES_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Dopamine transporter (DAT) 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 Quinoline yellow WS
                    Biological Activity IC50 = 29 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A3_HUMAN
            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) [6]
                    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) [6]
                    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) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Estrogen receptor alpha (ESR1) 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 Quinoline yellow WS
                    Biological Activity EC50 = 13156.33 nM (estimated based on the structural similarity with CHEMBL1417293 ) [7]
                    Structural Similarity Tanimoto coefficient = 0.828729282
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity IC50 = 18 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_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 ) [8]
                    Structural Similarity Tanimoto coefficient = 0.93081761
                    Tested Species Homo sapiens (Human)
                    UniProt ID TPOR_HUMAN
      Cell line (CELL)
            DBT Name: Leukemia K562 cells (K562) 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 Sodium stearyl fumarate
                    Biological Activity IC50 = 20.2 ug.mL-1 (estimated based on the structural similarity with CHEMBL3126829 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.75
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0004
            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 Sodium stearyl fumarate
                    Biological Activity IC50 = 60 ug.mL-1 (estimated based on the structural similarity with CHEMBL3126829 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.75
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0031
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Scientific perspectives on extending the provision for waivers of in vivo bioavailability and bioequivalence studies for drug products containing high solubility-low permeability drugs (BCS-Class 3). AAPS J. 2008 Jun;10(2):300-5.
3 Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
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.
5 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
6 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.
7 PubChem BioAssay data set.
8 Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis. J Med Chem. 2001 Oct 25; 44(22):3730-45.
9 Synthesis and evaluation of (-)-Massoialactone and analogues as potential anticancer and anti-inflammatory agents. Eur J Med Chem. 2014 Apr 9; 76:291-300.

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