General Information of DFM (ID: F05185)
Name	Cyclosporin A 25 mg capsule
Company	Mayne Pharma
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
	E0LT2O	DIG Info	Alpha-tocopherol	Antimicrobial preservative ...
	E09YYN	DIG Info	Eisenoxyd	Colorant
	E06WYP	DIG Info	Glycerin	Antimicrobial preservative ...
	E03VAV	DIG Info	Glyceryl monocaprylate	Emollient ...
	E04KSN	DIG Info	Hexahydric alcohol	Diluent ...
	E0X2OX	DIG Info	Medium-chain triglyceride	Emollient ...
	E0CX3L	DIG Info	Polyoxyl 35 castor oil	Emulsifying agent ...
	E05BSD	DIG Info	Titanium dioxide	Coating 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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	IC50 = 250 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN ; CP3A5_HUMAN ; CP3A7_HUMAN ; CP343_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	Inhibition (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	Polyoxyl 35 castor oil
Biological Activity	EC50 = 306.5 uM (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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 600 uM (tested by experiment)					[4]
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	Polyoxyl 35 castor oil
Biological Activity	EC50 = 113.3 uM (tested by experiment)					[3]
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	Polyoxyl 35 castor oil
Biological Activity	EC50 = 41.1 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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 30 uM (tested by experiment)					[4]
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	Polyoxyl 35 castor oil
Biological Activity	EC50 = 36.1 uM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2CJ_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	Polyoxyl 35 castor oil
Biological Activity	EC50 = 10.1 uM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A5_HUMAN
Transferase (TFase)
DBT Name: Glutathione S-transferase P (GSTP1)				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	Alpha-tocopherol
Biological Activity	IC50 = 500 nM (tested by experiment)					[5]
Tested Species	Homo sapiens (Human)
UniProt ID	GSTP1_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	Polyoxyl 35 castor oil
Biological Activity	EC50 = 1.1 uM (tested by experiment)					[3]
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	Polyoxyl 35 castor oil
Biological Activity	Inhibition ratio = 51 % (tested by experiment)					[6]
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	Polyoxyl 35 castor oil
Biological Activity	Inhibition ratio > 73 % (tested by experiment)					[7]
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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 5 mg.mL-1 (tested by experiment)					[8]
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	Polyoxyl 35 castor oil
Biological Activity	Inhibition ratio = 61 % (tested by experiment)					[9]
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	Polyoxyl 35 castor oil
Biological Activity	Inhibition ratio > 100 % (tested by experiment)					[10]
Tested Species	Homo sapiens (Human)
UniProt ID	MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
DBT Name: Urate exporter (BCRP)				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	Polyoxyl 35 castor oil
Biological Activity	Inhibition ratio > 40 % (tested by experiment)					[10]
Tested Species	Homo sapiens (Human)
UniProt ID	ABCG2_HUMAN
Potential-driven transporter (PDT)
DBT Name: Solute carrier SLCO1B1 (OATP-C)				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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.19 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO1B1_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.3 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO1B1_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.0011 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.0098 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_HUMAN
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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.00054 %(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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.00034 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO1A2_HUMAN
DBT Name: Organic anion transporter 8 (OAT8)				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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.001 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO1B3_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.0047 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	SO1B3_HUMAN
DBT Name: Sodium/bile acid cotransporter (SLC10A1)				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	Polyoxyl 35 castor oil
Biological Activity	IC50 = 2.8 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	NTCP_HUMAN
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	IC50 = 0.012 %(w/v) (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	NTCP_HUMAN
Cell line (CELL)
DBT Name: Colon cancer Caco-2 cells (Caco-2)				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	Medium-chain triglyceride
Biological Activity	Inhibition ratio > 36 % (tested by experiment)					[7]
Tested Species	Homo sapiens (Human)
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyoxyl 35 castor oil
Biological Activity	Chylomicron secretion downregulation (tested by experiment)					[12]
Tested Species	Homo sapiens (Human)

References
1	Nonionic surfactants are strong inhibitors of cytochrome P450 3A biotransformation activity in vitro and in vivo. Eur J Pharm Sci. 2009 Mar 2;36(4-5):401-11.
2	In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. iopharm Drug Dispos. 2004 Jan;25(1):37-49.
3	Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4	Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
5	Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example. J Med Chem. 2018 Sep 13; 61(17):7448-7470.
6	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.
7	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.
8	Reversal of multidrug resistance by surfactants. Br J Cancer. 1992 Jul;66(1):62-8.
9	A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci. 2002 Sep;91(9):1991-2002.
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.
12	The effects of pluronics block copolymers and Cremophor EL on intestinal lipoprotein processing and the potential link with P-glycoprotein in Caco-2 cells. Pharm Res. 2003 Jul;20(7):1085-92.

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