Details of the Drug Formulation (DFM)

General Information of DFM (ID: F05184)
Name
Cyclosporin A 25 mg capsule
Company
IVAX Pharmaceuticals
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
E02WLG DIG Info Aminoethanoic acid Buffering agent ...
E0VX5C DIG Info DL-alpha-tocopherol Antioxidant
E0L3MB DIG Info FD&C blue no. 2 Colorant
E0M0IE DIG Info Ferric hydroxide oxide yellow Colorant
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E04KSN DIG Info Hexahydric alcohol Diluent ...
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: Adenosine receptor A3 (AA3R) 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 FD&C blue no. 2
                    Biological Activity IC50 = 1 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AA3R_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Monoamine oxidase A (MAO-A) 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 FD&C blue no. 2
                    Biological Activity IC50 > 3 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID AOFA_HUMAN
            DBT Name: Prostaglandin G/H synthase 2 (COX-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 FD&C blue no. 2
                    Biological Activity IC50 = 24 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
            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
      Transferase (TFase)
            DBT Name: VEGF-2 receptor (KDR) 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 FD&C blue no. 2
                    Biological Activity IC50 = 3.1 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID VGFR2_HUMAN
      Hydrolase (HDase)
            DBT Name: Presenilin 1 (PSEN1) 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 DL-alpha-tocopherol
                    Biological Activity EC50 > 100000 nM (tested by experiment) [5]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PSN1_HUMAN
            DBT Name: Protein-tyrosine phosphatase 1D (PTPN11) 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 FD&C blue no. 2
                    Biological Activity IC50 = 7940 nM (estimated based on the structural similarity with CHEMBL3692077 ) [6]
                    Structural Similarity Tanimoto coefficient = 0.822222222
                    Tested Species Homo sapiens (Human)
                    UniProt ID PTN11_HUMAN
      Lyase/isomerase/ligase (L/I/G)
            DBT Name: Serine racemase (SRR) 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 Aminoethanoic acid
                    Biological Activity Ki = 366000 nM (tested by experiment) [7]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SRR_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Glycine type-1 transporter (GlyT-1) 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 Aminoethanoic acid
                    Biological Activity IC50 = 31600 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A9_HUMAN
            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 FD&C blue no. 2
                    Biological Activity Inhibition ratio = 26 % (tested by experiment) [9]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Glutamate receptor NMDA (GRIN) 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 Aminoethanoic acid
                    Biological Activity Ki = 125.89 nM (tested by experiment) [10]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID NMDZ1_RAT ; NMDE1_RAT ; NMDE2_RAT ; NMDE3_RAT ; NMDE4_RAT ; NMD3A_RAT ; NMD3B_RAT
            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 Aminoethanoic acid
                    Biological Activity EC50 = 94000 nM (tested by experiment) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID GLRA1_HUMAN
      Nuclear receptor (NR)
            DBT Name: Estrogen receptor alpha (ESR1) 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 FD&C blue no. 2
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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.
5 Membrane anchoring -secretase modulators with terpene-derived moieties. Bioorg Med Chem Lett. 2013 Jul 1; 23(13):3852-6.
6 US patent application no. 8987474B2, Inhibition of Shp2/PTPN11 Protein Tyrosine Phosphatase by NSC-87877, NSC-117199 and Their Analogs.
7 In silico and pharmacological screenings identify novel serine racemase inhibitors. Bioorg Med Chem Lett. 2014 Aug 15; 24(16):3732-5.
8 Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 1: development of a potent and CNS penetrant [3.1.0]-based lead. Bioorg Med Chem Lett. 2014 Feb 15; 24(4):1067-70.
9 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.
10 Drug design, in vitro pharmacology, and structure-activity relationships of 3-acylamino-2-aminopropionic acid derivatives, a novel class of partial agonists at the glycine site on the N-methyl-D-aspartate (NMDA) receptor complex. J Med Chem. 2009 Aug 27; 52(16):5093-107.
11 Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor. J Med Chem. 2007 Sep 20; 50(19):4616-29.

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