General Information of DFM (ID: F23411)
Name
Cyclosporine 100mg/ml solution
Company
Novartis
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
E0SF4Y DIG Info Ethanol Antimicrobial preservative ...
E00PSA DIG Info Glyceryl monooleate Bioadhesive material ...
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      Transferase (TFase)
            DBT Name: Diacylglycerol kinase alpha (DGKA) 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 Glyceryl monooleate
                    Biological Activity Ki = 91000 nM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DGKA_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 for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Glyceryl monooleate
                    Biological Activity Inhibition ratio = 62 % (tested by experiment) [2]
                    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 Glyceryl monooleate
                    Biological Activity Protein expression downregulation = 39.1 % (tested by experiment) [3]
                    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 Glyceryl monooleate
                    Biological Activity Inhibition ratio = 39 % (tested by experiment) [3]
                    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 Glyceryl monooleate
                    Biological Activity Inhibition ratio = 63 % (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
References
1 Identification of a novel DGKalpha inhibitor for XLP-1 therapy by virtual screening. Eur J Med Chem. 2019; 164:378-390.
2 Effects of monoglycerides on rhodamine 123 accumulation, estradiol 17 beta-D-glucuronide bidirectional transport and MRP2 protein expression within Caco-2 cells. J Pharm Pharm Sci. 2008;11(3):45-62.
3 Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm. Sep-Oct 2008;5(5):863-75.

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