General Information of DFM (ID: F05182)
Name	Cyclosporin A 25 mg capsule
Company	Teva 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
	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 ...
	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 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	Hydrogenated polyoxyl 40 castor oil
Biological Activity	IC50 = 800 uM (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 = 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)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2C9_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)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	PSN1_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)					[5]
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)					[6]
Tested Species	Homo sapiens (Human)
UniProt ID	SC6A9_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)					[7]
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)					[8]
Tested Species	Homo sapiens (Human)
UniProt ID	GLRA1_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	Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
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	Membrane anchoring -secretase modulators with terpene-derived moieties. Bioorg Med Chem Lett. 2013 Jul 1; 23(13):3852-6.
5	In silico and pharmacological screenings identify novel serine racemase inhibitors. Bioorg Med Chem Lett. 2014 Aug 15; 24(16):3732-5.
6	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.
7	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.
8	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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