General Information of DFM (ID: F23410)
Name	Cyclosporine 25mg capsule
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
	E07VCZ	DIG Info	Carmine	Colorant
	E0VX5C	DIG Info	DL-alpha-tocopherol	Antioxidant
	E0SF4Y	DIG Info	Ethanol	Antimicrobial preservative ...
	E0T2WF	DIG Info	Ferric oxide black	Colorant
	E00FTX	DIG Info	Gelatin	Other agent
	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 ...
	E0I4VY	DIG Info	Triolein	Complexing agent ...

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	Propylene glycol
Biological Activity	Inhibition ratio < 20 % (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
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	Gelatin
Biological Activity	IC50 = 141.2 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	Gelatin
Biological Activity	EC50 = 249.5 uM (tested by experiment)					[4]
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	Hydrogenated polyoxyl 40 castor oil
Biological Activity	IC50 = 30 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	Gelatin
Biological Activity	EC50 = 20.5 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	Gelatin
Biological Activity	EC50 = 379.9 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2D6_HUMAN
Hydrolase (HDase)
DBT Name: Oleamide hydrolase 1 (FAAH)				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	Triolein
Biological Activity	IC50 = 11000 nM (estimated based on the structural similarity with CHEMBL230967 )					[5]
Structural Similarity	Tanimoto coefficient = 0.93442623
Tested Species	Rattus norvegicus (Rat)
UniProt ID	FAAH1_RAT
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)					[6]
Tested Species	Homo sapiens (Human)
UniProt ID	PSN1_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	Gelatin
Biological Activity	IC50 = 40.9 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	CP1A2_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 for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Carmine
Biological Activity	Inhibition ratio = 29.4 % (tested by experiment)					[7]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_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	Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase. J Med Chem. 2007 Oct 4; 50(20):5012-23.
6	Membrane anchoring -secretase modulators with terpene-derived moieties. Bioorg Med Chem Lett. 2013 Jul 1; 23(13):3852-6.
7	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.

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