Details of the Drug Formulation (DFM)

General Information of DFM (ID: F19239)
Name
Risperidone 4 mg tablet
Company
Sandoz
Active Pharmaceutical Ingredient (API) Risperidone API Info click to show the detail info of this API
Schizophrenia ICD-11: 6A20 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0TU6R DIG Info Acesulfame Flavoring agent
E0BI3X DIG Info Aspartame Flavoring agent
E0F2PK DIG Info Calcium stearate lubricant
E03SQI DIG Info Carmellose sodium Disintegrant
E0NN4I DIG Info Dextrin Binding agent ...
E09YYN DIG Info Eisenoxyd Colorant
E0Q6DQ DIG Info Mannitol Diluent ...
E0FU3S DIG Info Monoammonium glycyrrhizate Emulsifying agent ...
E0Q3PU DIG Info Saccharose Binding agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            DBT Name: Dehydrogenase/reductase 9C 3 (11-DH2) 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 Monoammonium glycyrrhizate
                    Biological Activity IC50 = 0.4 nM (estimated based on the structural similarity with CHEMBL441687 ) [1]
                    Structural Similarity Tanimoto coefficient = 0.982905983
                    Tested Species Homo sapiens (Human)
                    UniProt ID DHI2_HUMAN
            DBT Name: Dehydrogenase/reductase 26C 1 (11-DH) 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 Monoammonium glycyrrhizate
                    Biological Activity EC50 = 10 nM (estimated based on the structural similarity with CHEMBL441687 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.982905983
                    Tested Species Homo sapiens (Human)
                    UniProt ID DHI1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Monoammonium glycyrrhizate
                    Biological Activity EC50 = 8 nM (estimated based on the structural similarity with CHEMBL441687 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.982905983
                    Tested Species Mus musculus (Mouse)
                    UniProt ID DHI1_MOUSE
            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 Carmellose sodium
                    Biological Activity Protein expression upregulation (tested by experiment) [3]
                    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 Carmellose sodium
                    Biological Activity Protein expression upregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Matrix metalloproteinase-1 (MMP1) 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 Aspartame
                    Biological Activity IC50 = 20000 nM (estimated based on the structural similarity with CHEMBL62186 ) [4]
                    Structural Similarity Tanimoto coefficient = 0.916666667
                    Tested Species Homo sapiens (Human)
                    UniProt ID MMP1_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase II (CA2) 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 Acesulfame
                    Biological Activity Ki > 20000 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH2_HUMAN
            DBT Name: Carbonic anhydrase IX (CA9) 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 Acesulfame
                    Biological Activity Ki = 2400 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH9_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 Monoammonium glycyrrhizate
                    Biological Activity Inhibition ratio = 41.4 % (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Glycine receptor alpha-1 (GLRA1) 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 Mannitol
                    Biological Activity EC50 = 12589.25 nM (estimated based on the structural similarity with CHEMBL604608 ) [7]
                    Structural Similarity Tanimoto coefficient = 0.804878049
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Pregnane X receptor (NR1I2) 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 Aspartame
                    Biological Activity Ki = 13 uM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NR1I2_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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Dextrin
                    Biological Activity Inhibition ratio > 55 % (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
            DBT Name: Immortalized MDCK cells (MDCK) 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 Monoammonium glycyrrhizate
                    Biological Activity EC50 = 15200 nM (estimated based on the structural similarity with CHEMBL441687 ) [10]
                    Structural Similarity Tanimoto coefficient = 0.982905983
                    Tested Species Canis lupus familiaris (Dog)
                    Cellosaurus ID CVCL_0422
References
1 Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11-hydroxysteroid dehydrogenases. J Nat Prod. 2012 Apr 27; 75(4):599-604.
2 Synthesis and evaluation of piperidine urea derivatives as efficacious 11-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice. Bioorg Med Chem Lett. 2012 Apr 15; 22(8):2748-52.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket. Bioorg Med Chem Lett. (1997) 7:193-198.
5 Sweet Binders: Carbonic Anhydrase IX in Complex with Sucralose. ACS Med Chem Lett. 2018 May 10; 9(7):657-661.
6 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.
7 Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
8 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
9 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.
10 Glycyrrhizic acid derivatives as influenza A/H1N1 virus inhibitors. Bioorg Med Chem Lett. 2015 Apr 15; 25(8):1742-1746.

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