General Information of DFM (ID: F11297)
Name	Lansoprazole 15 mg tablet
Company	Takeda Pharmaceuticals America
Active Pharmaceutical Ingredient (API)	Lansoprazole		API Info click to show the detail info of this API
	Duodenal ulcer		ICD-11: DA63	Approved
Drug Inactive Ingredient (DIGs)
	DIG ID	DIG Info	DIG Name	DIG Functional Class
	E0BI3X	DIG Info	Aspartame	Flavoring agent
	E09QIG	DIG Info	Citric acid monohydrate	Acidulant ...
	E09YYN	DIG Info	Eisenoxyd	Colorant
	E0H2RX	DIG Info	Glyceryl monostearate	Emollient ...
	E00DHW	DIG Info	Lactose monohydrate	Binding agent ...
	E04NDE	DIG Info	Magnesium carbonate	Adsorbent ...
	E01UTP	DIG Info	Magnesium stearate	lubricant
	E0Q6DQ	DIG Info	Mannitol	Diluent ...
	E0R4JL	DIG Info	Polysorbate 80	Dispersing agent ...
	E0QY1F	DIG Info	Talc	Anticaking agent ...
	E05BSD	DIG Info	Titanium dioxide	Coating agent ...
	E0K0OU	DIG Info	Triethyl citrate	Plasticizing agent ...

Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
G-protein coupled receptor (GPCR)
DBT Name: Adenosine receptor A3 (AA3R)				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	Polysorbate 80
Biological Activity	IC50 = 9.3 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	AA3R_HUMAN
DBT Name: Muscarinic receptor M1 (ACM1)				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	Polysorbate 80
Biological Activity	IC50 = 2.6 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ACM1_HUMAN
DBT Name: Muscarinic receptor M2 (ACM2)				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	Polysorbate 80
Biological Activity	IC50 = 1.3 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ACM2_HUMAN
DBT Name: Dopamine D3 receptor (DRD3)				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	Polysorbate 80
Biological Activity	IC50 = 22 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	DRD3_HUMAN
DBT Name: Histamine H3 receptor (HRH3)				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	Polysorbate 80
Biological Activity	IC50 = 5.3 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	HRH3_HUMAN
DBT Name: Thromboxane A2 receptor (TBXA2R)				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	Polysorbate 80
Biological Activity	IC50 = 12 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	TA2R_HUMAN
Oxidoreductase (ORase)
DBT Name: Prostaglandin G/H synthase 1 (COX-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	Polysorbate 80
Biological Activity	IC50 = 1 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PGH1_HUMAN
DBT Name: Prostaglandin G/H synthase 2 (COX-2)				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	Polysorbate 80
Biological Activity	IC50 = 2.9 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PGH2_HUMAN
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	Polysorbate 80
Biological Activity	Inhibition (tested by experiment)					[2]
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	Polysorbate 80
Biological Activity	Protein expression downregulation (tested by experiment)					[3]
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	Magnesium stearate
Biological Activity	Protein expression downregulation (tested by experiment)					[4]
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	Polysorbate 80
Biological Activity	IC50 = 201 uM (tested by experiment)					[5]
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	Polysorbate 80
Biological Activity	IC50 = 400 uM (tested by experiment)					[6]
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	Polysorbate 80
Biological Activity	Protein expression downregulation (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	Polysorbate 80
Biological Activity	IC50 = 225 uM (tested by experiment)					[5]
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	Polysorbate 80
Biological Activity	EC50 = 374.2 uM (tested by experiment)					[5]
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	Polysorbate 80
Biological Activity	IC50 = 40 uM (tested by experiment)					[6]
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	Polysorbate 80
Biological Activity	IC50 = 118.6 uM (tested by experiment)					[5]
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	Polysorbate 80
Biological Activity	EC50 = 486.4 uM (tested by experiment)					[5]
Tested Species	Homo sapiens (Human)
UniProt ID	CP2D6_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	Polysorbate 80
Biological Activity	IC50 = 186.4 uM (tested by experiment)					[5]
Tested Species	Homo sapiens (Human)
UniProt ID	CP3A5_HUMAN
Hydrolase (HDase)
DBT Name: Matrix metalloproteinase-1 (MMP1)				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	Aspartame
Biological Activity	IC50 = 20000 nM (estimated based on the structural similarity with CHEMBL62186 )					[7]
Structural Similarity	Tanimoto coefficient = 0.916666667
Tested Species	Homo sapiens (Human)
UniProt ID	MMP1_HUMAN
DBT Name: Phosphodiesterase 3A (PDE3A)				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	Polysorbate 80
Biological Activity	IC50 > 3 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PDE3A_HUMAN
DBT Name: Phosphodiesterase 4D (PDE4D)				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	Polysorbate 80
Biological Activity	IC50 > 10 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PDE4D_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 for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Glyceryl monostearate
Biological Activity	Inhibition ratio = 76 % (tested by experiment)					[8]
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	Glyceryl monostearate
Biological Activity	Protein expression downregulation = 52.3 % (tested by experiment)					[9]
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	Glyceryl monostearate
Biological Activity	Inhibition ratio = 46 % (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	Glyceryl monostearate
Biological Activity	Inhibition ratio = 47 % (tested by experiment)					[9]
Tested Species	Homo sapiens (Human)
UniProt ID	MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polysorbate 80
Biological Activity	IC50 = 0.31 mg.mL-1 (tested by experiment)					[10]
Tested Species	Homo sapiens (Human)
UniProt ID	MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polysorbate 80
Biological Activity	Inhibition ratio = 60 % (tested by experiment)					[11]
Tested Species	Homo sapiens (Human)
UniProt ID	MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
Experiment (6) for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polysorbate 80
Biological Activity	Inhibition ratio > 250 % (tested by experiment)					[12]
Tested Species	Homo sapiens (Human)
UniProt ID	MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_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 )					[13]
Structural Similarity	Tanimoto coefficient = 0.804878049
Tested Species	Homo sapiens (Human)
UniProt ID	GLRA1_HUMAN
Nuclear receptor (NR)
DBT Name: Estrogen receptor alpha (ESR1)				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	Polysorbate 80
Biological Activity	IC50 > 10 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	ESR1_HUMAN
DBT Name: Pregnane X receptor (NR1I2)				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	Aspartame
Biological Activity	Ki = 13 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	NR1I2_HUMAN
DBT Name: Progesterone receptor (PGR)				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	Polysorbate 80
Biological Activity	IC50 = 21 uM (tested by experiment)					[1]
Tested Species	Homo sapiens (Human)
UniProt ID	PRGR_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 for Assessing the Biological Activity of the Studied DIG on This DBT
Interacting DIG	Polysorbate 80
Biological Activity	Chylomicron secretion upregulation (tested by experiment)					[14]
Tested Species	Homo sapiens (Human)
DBT Name: Prostate cancer LNCaP cells (LNCaP)				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	Glyceryl monostearate
Biological Activity	IC50 > 100000 nM (tested by experiment)					[15]
Tested Species	Homo sapiens (Human)
Cellosaurus ID	CVCL_0395

References
1	The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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	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.
4	Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5	Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
6	Effects of non-ionic surfactants on cytochrome P450-mediated metabolism in vitro. Eur J Pharm Biopharm. 2011 May;78(1):166-72.
7	Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket. Bioorg Med Chem Lett. (1997) 7:193-198.
8	Effects of monoglycerides on rhodamine 123 accumulation, estradiol 17 beta-D-glucuronide bidirectional transport and MRP2 protein expression within Caco-2 cells. J Pharm Pharm Sci. 2008;11(3):45-62.
9	Effects of monoglycerides on P-glycoprotein: modulation of the activity and expression in Caco-2 cell monolayers. Mol Pharm. Sep-Oct 2008;5(5):863-75.
10	Reversal of multidrug resistance by surfactants. Br J Cancer. 1992 Jul;66(1):62-8.
11	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.
12	Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release. 2007 Dec 4;124(1-2):1-5.
13	Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective. Bioorg Med Chem Lett. 2017 Jun 1; 27(11):2239-2258.
14	Stimulation of triglyceride-rich lipoprotein secretion by polysorbate 80: in vitro and in vivo correlation using Caco-2 cells and a cannulated rat intestinal lymphatic model. Pharm Res. 2004 Dec;21(12):2320-6.
15	Lignanamides and nonalkaloidal components of Hyoscyamus niger seeds. J Nat Prod. 2002 Feb; 65(2):206-9.

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