General Information of DFM (ID: F05265)
Name	Darunavir 400 mg tablet
Company	RemedyRepack
Active Pharmaceutical Ingredient (API)	Darunavir		API Info click to show the detail info of this API
	Human immunodeficiency virus infection		ICD-11: 1C60	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E0PE9M	DIG Info	Crospovidone	Disintegrant
	E01UTP	DIG Info	Magnesium stearate	lubricant
	E09IPB	DIG Info	Polyethylene glycol 3350	Coating agent ...
	E0V3ER	DIG Info	Polyvinyl alcohol	Coating agent ...
	E01UTV	DIG Info	Silicon dioxide	Anticaking agent ...
	E0L0MR	DIG Info	Sunset yellow FCF	Colorant
	E0QY1F	DIG Info	Talc	Anticaking 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: 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	Magnesium stearate
Biological Activity	Protein expression downregulation (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	Crospovidone
Biological Activity	Protein expression downregulation (tested by experiment)					[1]
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	Polyethylene glycol 3350
Biological Activity	Protein expression upregulation (tested by experiment)					[1]
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	Silicon dioxide
Biological Activity	Protein expression downregulation (tested by experiment)					[1]
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	Polyvinyl alcohol
Biological Activity	IC50 = 548.9 uM (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2E1_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	Polyvinyl alcohol
Biological Activity	EC50 = 354.8 uM (tested by experiment)					[2]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2D6_HUMAN
Primary active transporter (PAT)
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 for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polyethylene glycol 3350
Biological Activity	Protein expression downregulation (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	MDR1_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Sunset yellow FCF
Biological Activity	Inhibition ratio = 54.5 % (tested by experiment)					[3]
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	Sunset yellow FCF
Biological Activity	Ki = 68.4 uM (tested by experiment)					[3]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_HUMAN
Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Sunset yellow FCF
Biological Activity	Ki = 74 uM (tested by experiment)					[4]
Tested Species	Homo sapiens (Human)
UniProt ID	SO2B1_HUMAN
Other protein families (OPF)
DBT Name: Thrombopoietin receptor (MPL)				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	Sunset yellow FCF
Biological Activity	EC50 = 3000 nM (estimated based on the structural similarity with CHEMBL122867 )					[5]
Structural Similarity	Tanimoto coefficient = 0.93081761
Tested Species	Homo sapiens (Human)
UniProt ID	TPOR_HUMAN

References
1	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
2	Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
3	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.
4	The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
5	Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis. J Med Chem. 2001 Oct 25; 44(22):3730-45.

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