Details of the Drug Formulation (DFM)

General Information of DFM (ID: F18023)
Name
Promethazine 50 mg tablet
Company
Physicians Total Care
Active Pharmaceutical Ingredient (API) Promethazine API Info click to show the detail info of this API
Allergic rhinitis ICD-11: CA08 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E06RUT DIG Info D&C red no. 27 Colorant
E01VHX DIG Info D&C red no. 30 Colorant
E0T4YW DIG Info Hypromellose Coating agent
E00DHW DIG Info Lactose monohydrate Binding agent ...
E01UTP DIG Info Magnesium stearate lubricant
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 Hypromellose
                    Biological Activity Protein expression upregulation (tested by experiment) [1]
                    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 Hypromellose
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
            DBT Name: Cytochrome P450 2E1 (CYP2E1) 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 Hypromellose
                    Biological Activity IC50 = 253.5 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) 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 Hypromellose
                    Biological Activity EC50 = 211.8 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2CJ_HUMAN
            DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) 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 Hypromellose
                    Biological Activity EC50 = 159.3 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2D6_HUMAN
            DBT Name: Cytochrome P450 3A5 (CYP3A5) 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 Hypromellose
                    Biological Activity IC50 = 19.4 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A5_HUMAN
      Transferase (TFase)
            DBT Name: Arginine methyltransferase 1 (PRMT1) 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 D&C red no. 27
                    Biological Activity IC50 = 1400 nM (estimated based on the structural similarity with CHEMBL376503 ) [3]
                    Structural Similarity Tanimoto coefficient = 0.781914894
                    Tested Species Homo sapiens (Human)
                    UniProt ID ANM1_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Cholesterol 25-hydroxylase (CYP1A2) 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 Hypromellose
                    Biological Activity EC50 = 106.7 uM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C red no. 27
                    Biological Activity Inhibition ratio = 69 % (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG D&C red no. 27
                    Biological Activity Ki = 1 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Other protein families (OPF)
            DBT Name: Heat shock factor 1 (HSF1) 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 D&C red no. 30
                    Biological Activity EC50 = 9054 nM (estimated based on the structural similarity with CHEMBL1339303 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.776859504
                    Tested Species Mus musculus (Mouse)
                    UniProt ID HSF1_MOUSE
            DBT Name: Nuclear factor-kappa B (NFKB) 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 D&C red no. 30
                    Biological Activity EC50 = 122869 nM (estimated based on the structural similarity with CHEMBL1339303 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.776859504
                    Tested Species Homo sapiens (Human)
                    UniProt ID NFKB1_HUMAN ; NFKB2_HUMAN ; TF65_HUMAN
      Cell line (CELL)
            DBT Name: Colon cancer Caco-2 cells (Caco-2) 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 Hypromellose
                    Biological Activity Promotion ratio > 18 % (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Hypromellose
                    Biological Activity Promotion ratio > 27 % (tested by experiment) [6]
                    Tested Species Homo sapiens (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 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3 Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations. J Med Chem. 2007 Mar 22; 50(6):1241-53.
4 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.
5 PubChem BioAssay data set.
6 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.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.