Details of the Drug Formulation (DFM)

General Information of DFM (ID: F02618)
Name
Bisacodyl 5 mg tablet
Company
Spirit Pharmaceutical
Active Pharmaceutical Ingredient (API) Bisacodyl API Info click to show the detail info of this API
Irritable bowel syndrome ICD-11: DD91 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E01UTP DIG Info Magnesium stearate lubricant
E0V6QI DIG Info methylparaben Antimicrobial preservative
E0Q3PU DIG Info Saccharose Binding agent ...
E0L0MR DIG Info Sunset yellow FCF Colorant
E0QY1F DIG Info Talc Anticaking agent ...
E0FU1S DIG Info Vinylpyrrolidone Binding agent ...
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 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
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Carbonic anhydrase I (CA1) 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 methylparaben
                    Biological Activity Ki = 2600 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH1_HUMAN
            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 methylparaben
                    Biological Activity Ki = 3400 nM (tested by experiment) [2]
                    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 methylparaben
                    Biological Activity Ki = 5500 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH9_HUMAN
            DBT Name: Carbonic anhydrase VII (CA7) 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 methylparaben
                    Biological Activity Ki = 780 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH7_HUMAN
            DBT Name: Carbonic anhydrase XII (CA12) 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 methylparaben
                    Biological Activity Ki = 820 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH12_HUMAN
            DBT Name: Carbonic anhydrase XIV (CA14) 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 methylparaben
                    Biological Activity Ki = 4100 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CAH14_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 Sunset yellow FCF
                    Biological Activity Inhibition ratio = 54.5 % (tested by experiment) [3]
                    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 Sunset yellow FCF
                    Biological Activity Ki = 68.4 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Sunset yellow FCF
                    Biological Activity Ki = 74 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Androgen receptor (AR) 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 methylparaben
                    Biological Activity IC50 > 426579.52 nM (tested by experiment) [5]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID ANDR_RAT
      Other protein families (OPF)
            DBT Name: Thrombopoietin receptor (MPL) 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 Sunset yellow FCF
                    Biological Activity EC50 = 3000 nM (estimated based on the structural similarity with CHEMBL122867 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.93081761
                    Tested Species Homo sapiens (Human)
                    UniProt ID TPOR_HUMAN
      Cell line (CELL)
            DBT Name: Lung cancer A-549 cells (A-549) 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 methylparaben
                    Biological Activity IC50 > 20 ug.mL-1 (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0023
            DBT Name: Hepatoblastoma HepG2 cells (HepG2) 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 methylparaben
                    Biological Activity IC50 > 20 ug.mL-1 (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0027
            DBT Name: Cervical cancer KB cells (KB) 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 methylparaben
                    Biological Activity IC50 > 200000 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0372
            DBT Name: Carcinoma MDA-MB-231 cells (MDA-MB-231) 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 methylparaben
                    Biological Activity IC50 > 20 ug.mL-1 (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0062
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 Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV. Bioorg Med Chem. 2013 Mar 15; 21(6):1564-9.
3 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.
4 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
5 Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals. J Med Chem. 2005 Sep 8; 48(18):5666-74.
6 Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis. J Med Chem. 2001 Oct 25; 44(22):3730-45.
7 Bioactive Phenolic Components from the Twigs of Atalantia buxifolia. J Nat Prod. 2018 Jul 27; 81(7):1534-1539.
8 Synthesis and biological evaluation of 12 allenic aromatic ethers. Bioorg Med Chem Lett. 2007 May 15; 17(10):2785-8.

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