Details of the Drug Formulation (DFM)

General Information of DFM (ID: F07919)
Name
Felodipine 2.5 mg tablet
Company
Ranbaxy Pharmaceuticals
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
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E0L3MB DIG Info FD&C blue no. 2 Colorant
E0M0IE DIG Info Ferric hydroxide oxide yellow Colorant
E0RS6F DIG Info Sodium stearyl fumarate lubricant
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: Adenosine receptor A3 (AA3R) 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 FD&C blue no. 2
                    Biological Activity IC50 = 1 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Monoamine oxidase A (MAO-A) 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 FD&C blue no. 2
                    Biological Activity IC50 > 3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AOFA_HUMAN
            DBT Name: Prostaglandin G/H synthase 2 (COX-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 FD&C blue no. 2
                    Biological Activity IC50 = 24 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
      Transferase (TFase)
            DBT Name: VEGF-2 receptor (KDR) 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 FD&C blue no. 2
                    Biological Activity IC50 = 3.1 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID VGFR2_HUMAN
      Hydrolase (HDase)
            DBT Name: Protein-tyrosine phosphatase 1D (PTPN11) 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 FD&C blue no. 2
                    Biological Activity IC50 = 7940 nM (estimated based on the structural similarity with CHEMBL3692077 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.822222222
                    Tested Species Homo sapiens (Human)
                    UniProt ID PTN11_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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 2
                    Biological Activity Inhibition ratio = 26 % (tested by experiment) [3]
                    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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG FD&C blue no. 2
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_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 ) [4]
                    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 ) [4]
                    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 US patent application no. 8987474B2, Inhibition of Shp2/PTPN11 Protein Tyrosine Phosphatase by NSC-87877, NSC-117199 and Their Analogs.
3 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.
4 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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