Details of the Drug Formulation (DFM)

General Information of DFM (ID: F05179)
Name
Cyclosporin A 25 mg capsule
Company
Eon Labs
Active Pharmaceutical Ingredient (API) Cyclosporin A API Info click to show the detail info of this API
Rheumatoid arthritis ICD-11: FA20 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E04KSN DIG Info Hexahydric alcohol Diluent ...
E0VK1L DIG Info Hydrogenated polyoxyl 40 castor oil Emulsifying agent ...
E0PC2L DIG Info Polyethylene glycol 400 Coating agent ...
E01NLA DIG Info Tocophersolan Antioxidant ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Oxidoreductase (ORase)
            DBT Name: Cytochrome P450 3A (CYP3A) 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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity Protein expression downregulation (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
            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 Polyethylene glycol 400
                    Biological Activity IC50 = 10.77 mg.mL-1 (tested by experiment) [2]
                    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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 800 uM (tested by experiment) [3]
                    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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 0.25 mg.mL-1 (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocophersolan
                    Biological Activity EC50 = 28.3 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
               Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocophersolan
                    Biological Activity IC50 = 150 uM (tested by experiment) [3]
                    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 Tocophersolan
                    Biological Activity IC50 = 547.3 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2E1_HUMAN
            DBT Name: Cytochrome P450 2C9 (CYP2C9) 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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 30 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocophersolan
                    Biological Activity EC50 = 40.1 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocophersolan
                    Biological Activity IC50 = 300 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_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 Tocophersolan
                    Biological Activity EC50 = 114.8 uM (tested by experiment) [4]
                    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 Tocophersolan
                    Biological Activity IC50 = 84 uM (tested by experiment) [4]
                    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 Tocophersolan
                    Biological Activity EC50 = 420.6 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A5_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 Tocophersolan
                    Biological Activity EC50 = 208.8 uM (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 67 % (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MRP2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity Inhibition ratio > 73 % (tested by experiment) [6]
                    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 Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 28 % (tested by experiment) [7]
                    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 Polyethylene glycol 400
                    Biological Activity Inhibition ratio = 64 % (tested by experiment) [8]
                    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 Tocophersolan
                    Biological Activity Inhibition ratio = 50 % (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Tocophersolan
                    Biological Activity Inhibition ratio > 200 % (tested by experiment) [10]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Solute carrier SLCO1A2 (OATP-A) 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 Polyethylene glycol 400
                    Biological Activity IC50 = 0.14 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Polyethylene glycol 400
                    Biological Activity IC50 = 0.05 %(w/v) (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO1A2_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 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
3 Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
4 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
5 Inhibition of human efflux transporter ABCC2 (MRP2) by self-emulsifying drug delivery system: influences of concentration and combination of excipients. J Pharm Pharm Sci. 2014;17(4):447-60.
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.
7 The effect of polyoxyethylene polymers on the transport of ranitidine in Caco-2 cell monolayers. Int J Pharm. 2011 May 16;409(1-2):164-8.
8 Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm. 2006 Apr 26;313(1-2):49-56.
9 Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. Pharm Res. 1999 Dec;16(12):1812-7.
10 Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release. 2007 Dec 4;124(1-2):1-5.
11 Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012 Sep 4;9(9):2577-81.

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