Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET06RWH)
Name
Cytochrome P450 3A (CYP3A)
Family Oxidoreductase (ORase)  >>  Oxygen paired donor oxidoreductase (EC 1.14)
Organism
Homo sapiens (Human)
UniProt ID CP3A4_HUMAN (click to find more protein-related data of this DBT)
CP3A5_HUMAN (click to find more protein-related data of this DBT)
CP3A7_HUMAN (click to find more protein-related data of this DBT)
CP343_HUMAN (click to find more protein-related data of this DBT)
TTD ID T67977 (click to find more therapeutic target data of this DBT)
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Hydrogenated polyoxyl 40 castor oil Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Protein expression downregulation (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
          DIG Name: Poloxamer 188 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 750 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
          DIG Name: Polyoxyl 35 castor oil Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 250 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
          DIG Name: Polyoxyl 40 stearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 6800 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
          DIG Name: Polysorbate 20 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 320 uM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
          DIG Name: Polysorbate 80 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Protein expression downregulation (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
          DIG Name: Polyoxyl 15 hydroxystearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Inhibition (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
References
1 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.
2 Nonionic surfactants are strong inhibitors of cytochrome P450 3A biotransformation activity in vitro and in vivo. Eur J Pharm Sci. 2009 Mar 2;36(4-5):401-11.
3 In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. iopharm Drug Dispos. 2004 Jan;25(1):37-49.

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