Details of the Drug Formulation (DFM)

General Information of DFM (ID: F11376)
Name
Letrozole 2.5 mg tablet
Company
Jiangsu Hengrui Medicine
Active Pharmaceutical Ingredient (API) Letrozole API Info click to show the detail info of this API
Breast cancer ICD-11: 2C60 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09YYN DIG Info Eisenoxyd Colorant
E02FBG DIG Info Ferrosoferric oxide Colorant
E00DHW DIG Info Lactose monohydrate Binding agent ...
E01UTP DIG Info Magnesium stearate lubricant
E0PC2L DIG Info Polyethylene glycol 400 Coating agent ...
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E05BSD DIG Info Titanium dioxide Coating agent ...
E0H2SC DIG Info Water Solvent
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 Polyethylene glycol 400
                    Biological Activity IC50 = 10.77 mg.mL-1 (tested by experiment) [2]
                    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) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_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) [3]
                    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) [4]
                    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) [5]
                    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) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Potential-driven transporter (PDT)
            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) [7]
                    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) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_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 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 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.
4 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.
5 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.
6 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.
7 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.

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