Details of the Drug Formulation (DFM)

General Information of DFM (ID: F05180)
Name
Cyclosporin A 25 mg capsule
Company
Cardinal Health; Novartis Pharmaceuticals Corporation
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
E0JP9O DIG Info Caprylic acid Emulsifying agent ...
E02FBG DIG Info Ferrosoferric oxide Colorant
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E0VK1L DIG Info Hydrogenated polyoxyl 40 castor oil Emulsifying agent ...
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E05BSD DIG Info Titanium dioxide Coating agent ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: GPCR84 receptor (GPR84) 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 Caprylic acid
                    Biological Activity Ki = 19600 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID GPR84_HUMAN
      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) [2]
                    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 Propylene glycol
                    Biological Activity Inhibition ratio < 20 % (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 Hydrogenated polyoxyl 40 castor oil
                    Biological Activity IC50 = 800 uM (tested by experiment) [4]
                    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) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_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 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) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP2C9_HUMAN
References
1 An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights. J Med Chem. 2020 Mar 12; 63(5):2391-2410.
2 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.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
4 Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.

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