Details of the Drug Formulation (DFM)

General Information of DFM (ID: F18128)
Name
Propranolol 160 mg capsule
Company
AvKARE; Breckenridge Pharmaceutical
Active Pharmaceutical Ingredient (API) Propranolol API Info click to show the detail info of this API
Migraine ICD-11: 8A80 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0A1CS DIG Info Ammonia Alkalizing agent
E0N6BJ DIG Info Diethyl phthalate Plasticizing agent ...
E09YYN DIG Info Eisenoxyd Colorant
E0L3MB DIG Info FD&C blue no. 2 Colorant
E0M0IE DIG Info Ferric hydroxide oxide yellow Colorant
E02FBG DIG Info Ferrosoferric oxide Colorant
E0PC2L DIG Info Polyethylene glycol 400 Coating agent ...
E0ND5Z DIG Info Potassium hydroxide Alkalizing agent
E0Q3PU DIG Info Saccharose Binding agent ...
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
            DBT Name: Albendazole monooxygenase (CYP3A4) 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 Polyethylene glycol 400
                    Biological Activity IC50 = 10.77 mg.mL-1 (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_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 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.822222222
                    Tested Species Homo sapiens (Human)
                    UniProt ID PTN11_HUMAN
            DBT Name: Phosphodiesterase 4D (PDE4D) 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 Diethyl phthalate
                    Biological Activity IC50 = 8.5 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_HUMAN
      Primary active transporter (PAT)
            DBT Name: Multidrug resistance protein 2 (ABCC2) 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 Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 67 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio > 73 % (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 28 % (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 64 % (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_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) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
            DBT Name: Solute carrier SLCO1A2 (OATP-A) 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 Polyethylene glycol 400
                    Biological Activity IC50 = 0.14 %(w/v) (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity IC50 = 0.05 %(w/v) (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_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: Lung cancer A-549 cells (A-549) 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 Diethyl phthalate
                    Biological Activity IC50 = 38000 nM (estimated based on the structural similarity with CHEMBL4071043 ) [10]
                    Structural Similarity Tanimoto coefficient = 0.970588235
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0023
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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 US patent application no. 8987474B2, Inhibition of Shp2/PTPN11 Protein Tyrosine Phosphatase by NSC-87877, NSC-117199 and Their Analogs.
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.
6 The effect of polyoxyethylene polymers on the transport of ranitidine in Caco-2 cell monolayers. Int J Pharm. 2011 May 16;409(1-2):164-8.
7 Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm. 2006 Apr 26;313(1-2):49-56.
8 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.
9 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.
10 Novel bioactive molecules from Lentzea violacea strain AS 08 using one strain-many compounds (OSMAC) approach. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2579-2582.

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