Details of the Drug Formulation (DFM)

General Information of DFM (ID: F21391)
Name
Topotecan 1 mg capsule
Company
GlaxoSmithKline
Active Pharmaceutical Ingredient (API) Topotecan API Info click to show the detail info of this API
Ovarian cancer ICD-11: 2C73 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09YYN DIG Info Eisenoxyd Colorant
E0H2RX DIG Info Glyceryl monostearate Emollient ...
E05BSD DIG Info Titanium dioxide Coating agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity Inhibition ratio = 76 % (tested by experiment) [1]
                    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 Glyceryl monostearate
                    Biological Activity Protein expression downregulation = 52.3 % (tested by experiment) [2]
                    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 Glyceryl monostearate
                    Biological Activity Inhibition ratio = 46 % (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monostearate
                    Biological Activity Inhibition ratio = 47 % (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Cell line (CELL)
            DBT Name: Prostate cancer LNCaP cells (LNCaP) 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 Glyceryl monostearate
                    Biological Activity IC50 > 100000 nM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0395
References
1 Effects of monoglycerides on rhodamine 123 accumulation, estradiol 17 beta-D-glucuronide bidirectional transport and MRP2 protein expression within Caco-2 cells. J Pharm Pharm Sci. 2008;11(3):45-62.
2 Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm. Sep-Oct 2008;5(5):863-75.
3 Lignanamides and nonalkaloidal components of Hyoscyamus niger seeds. J Nat Prod. 2002 Feb; 65(2):206-9.

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