General Information of DFM (ID: F22776)
Name	Zileuton 600 mg tablet
Company	Prasco
Active Pharmaceutical Ingredient (API)	Zileuton		API Info click to show the detail info of this API
	Asthma		ICD-11: CA23	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E0PE9M	DIG Info	Crospovidone	Disintegrant
	E09YYN	DIG Info	Eisenoxyd	Colorant
	E0EI2M	DIG Info	Glyceryl dibehenate	Binding agent ...
	E01UTP	DIG Info	Magnesium stearate	lubricant
	E0Q6DQ	DIG Info	Mannitol	Diluent ...
	E0Q7IF	DIG Info	Povidone	Binding agent ...
	E0M1JK	DIG Info	Propylene glycol	Antimicrobial preservative ...
	E0QY1F	DIG Info	Talc	Anticaking agent ...

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
Oxidoreductase (ORase)
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)					[1]
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	Magnesium stearate
Biological Activity	Protein expression downregulation (tested by experiment)					[2]
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	Crospovidone
Biological Activity	Protein expression downregulation (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Povidone
Biological Activity	IC50 = 107 uM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_HUMAN
Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Povidone
Biological Activity	Protein expression upregulation (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A4_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	Povidone
Biological Activity	IC50 = 78.3 uM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	CP1A2_HUMAN
Transmembrane channel/porin (TC/P)
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	Mannitol
Biological Activity	EC50 = 12589.25 nM (estimated based on the structural similarity with CHEMBL604608 )					[4]
Structural Similarity	Tanimoto coefficient = 0.804878049
Tested Species	Homo sapiens (Human)
UniProt ID	GLRA1_HUMAN

References
1	Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
2	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3	Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4	Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.

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