Details of the Drug Formulation (DFM)

General Information of DFM (ID: F11331)
Name
Lansoprazole 30 mg tablet
Company
Physicians Total Care
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
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E00ONP DIG Info Cinnamaldehyde Flavoring agent
E01TKQ DIG Info Cis-3-hexenyl acetate Flavoring agent
E0NN4I DIG Info Dextrin Binding agent ...
E01ZRI DIG Info Ethyl butyrate Flavoring agent
E00ONP DIG Info Ethyl isovalerate Flavoring agent
E0L9VB DIG Info Gamma-decalactone Flavoring agent
E04NDE DIG Info Magnesium carbonate Adsorbent ...
E01UTP DIG Info Magnesium stearate lubricant
E0OY4C DIG Info Methyl cinnamate Flavoring agent
E0Q3PU DIG Info Saccharose Binding agent ...
E01UTV DIG Info Silicon dioxide Anticaking 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: Free fatty acid receptor 3 (FFAR3) 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 Ethyl butyrate
                    Biological Activity EC50 = 10100 nM (estimated based on the structural similarity with CHEMBL62381 ) [1]
                    Structural Similarity Tanimoto coefficient = 0.807692308
                    Tested Species Homo sapiens (Human)
                    UniProt ID FFAR3_HUMAN
      Oxidoreductase (ORase)
            DBT Name: Arachidonate 5-lipoxygenase (ALOX5) 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 Ethyl isovalerate
                    Biological Activity IC50 = 35000 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID LOX5_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Cinnamaldehyde
                    Biological Activity IC50 = 35000 nM (tested by experiment) [2]
                    Tested Species Homo sapiens (Human)
                    UniProt ID LOX5_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) [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 Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_HUMAN
      Hydrolase (HDase)
            DBT Name: Histone deacetylase (HDAC) 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 Ethyl butyrate
                    Biological Activity IC50 = 140000 nM (estimated based on the structural similarity with CHEMBL62381 ) [4]
                    Structural Similarity Tanimoto coefficient = 0.807692308
                    Tested Species Homo sapiens (Human)
                    UniProt ID HDAC1_HUMAN ; HDAC2_HUMAN ; HDAC3_HUMAN ; HDAC4_HUMAN ; HDAC5_HUMAN ; HDAC6_HUMAN ; HDAC7_HUMAN ; HDAC8_HUMAN ; HDAC9_HUMAN
            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 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.916666667
                    Tested Species Homo sapiens (Human)
                    UniProt ID MMP1_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 Gamma-decalactone
                    Biological Activity IC50 = 110000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP1A2_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: Gamma-aminobutyric acid receptor (GABRA) 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 Ethyl isovalerate
                    Biological Activity IC50 = 2280 nM (estimated based on the structural similarity with CHEMBL285171 ) [7]
                    Structural Similarity Tanimoto coefficient = 0.756756757
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID GBRA1_RAT ; GBRA2_RAT ; GBRA3_RAT ; GBRA4_RAT ; GBRA5_RAT ; GBRA6_RAT ; GBRB1_RAT ; GBRB2_RAT ; GBRB3_RAT ; GBRD_RAT ; GBRE_RAT ; GBRG1_RAT ; GBRG2_RAT ; GBRG3_RAT ; GBRP_RAT ; Q91ZM7_RAT
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Cinnamaldehyde
                    Biological Activity IC50 = 2280 nM (estimated based on the structural similarity with CHEMBL285171 ) [7]
                    Structural Similarity Tanimoto coefficient = 0.756756757
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID GBRA1_RAT ; GBRA2_RAT ; GBRA3_RAT ; GBRA4_RAT ; GBRA5_RAT ; GBRA6_RAT ; GBRB1_RAT ; GBRB2_RAT ; GBRB3_RAT ; GBRD_RAT ; GBRE_RAT ; GBRG1_RAT ; GBRG2_RAT ; GBRG3_RAT ; GBRP_RAT ; Q91ZM7_RAT
            DBT Name: Wasabi receptor (TRPA1) 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 Ethyl isovalerate
                    Biological Activity EC50 = 8511.38 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPA1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Cinnamaldehyde
                    Biological Activity EC50 = 8511.38 nM (tested by experiment) [8]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPA1_HUMAN
               Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Ethyl isovalerate
                    Biological Activity EC50 = 61000 nM (tested by experiment) [8]
                    Tested Species Mus musculus (Mouse)
                    UniProt ID TRPA1_MOUSE
               Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Cinnamaldehyde
                    Biological Activity EC50 = 61000 nM (tested by experiment) [8]
                    Tested Species Mus musculus (Mouse)
                    UniProt ID TRPA1_MOUSE
               Experiment (5) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Cis-3-hexenyl acetate
                    Biological Activity EC50 = 13300 nM (estimated based on the structural similarity with CHEMBL2268549 ) [9]
                    Structural Similarity Tanimoto coefficient = 0.755555556
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID TRPA1_RAT
            DBT Name: Transient receptor potential p8 (TRPM8) 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 Ethyl isovalerate
                    Biological Activity IC50 > 500000 nM (tested by experiment) [10]
                    Tested Species Mus musculus (Mouse)
                    UniProt ID TRPM8_MOUSE
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Cinnamaldehyde
                    Biological Activity IC50 > 500000 nM (tested by experiment) [10]
                    Tested Species Mus musculus (Mouse)
                    UniProt ID TRPM8_MOUSE
      Nuclear receptor (NR)
            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) [11]
                    Tested Species Homo sapiens (Human)
                    UniProt ID NR1I2_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 Dextrin
                    Biological Activity Inhibition ratio > 55 % (tested by experiment) [12]
                    Tested Species Homo sapiens (Human)
            DBT Name: Leukemia HL-60 cells (HL-60) 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 Methyl cinnamate
                    Biological Activity IC50 = 35690 nM (estimated based on the structural similarity with CHEMBL318196 ) [13]
                    Structural Similarity Tanimoto coefficient = 0.972972973
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_0002
            DBT Name: Umbilical vein endothelial cells (HUVEC) 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 Methyl cinnamate
                    Biological Activity IC50 = 100 ug.mL-1 (estimated based on the structural similarity with CHEMBL1911048 ) [14]
                    Structural Similarity Tanimoto coefficient = 0.972972973
                    Tested Species Homo sapiens (Human)
                    Cellosaurus ID CVCL_2959
References
1 Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists. ACS Med Chem Lett. 2016 Mar 30; 7(6):579-83.
2 5-Lipoxygenase as a drug target: A review on trends in inhibitors structural design, SAR and mechanism based approach. Bioorg Med Chem. 2019 Sep 1; 27(17):3745-3759.
3 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
4 Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20; 46(24):5097-116.
5 Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket. Bioorg Med Chem Lett. (1997) 7:193-198.
6 Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors. J Med Chem. 2005 Jun 2; 48(11):3808-15.
7 Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones. J Med Chem. 1994 Jan 21; 37(2):275-86.
8 N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites. Eur J Med Chem. 2019 May 15; 170:141-156.
9 Effect of acyclic monoterpene alcohols and their derivatives on TRP channels. Bioorg Med Chem Lett. 2014 Dec 1; 24(23):5507-11.
10 Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. J Nat Prod. 2014 Feb 28; 77(2):285-97.
11 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
12 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.
13 Phytochemical investigation of labdane diterpenes from the rhizomes of Hedychium spicatum and their cytotoxic activity. Bioorg Med Chem Lett. 2009 Nov 1; 19(21):6078-81.
14 Novel natural product-based cinnamates and their thio and thiono analogs as potent inhibitors of cell adhesion molecules on human endothelial cells. Eur J Med Chem. 2011 Nov; 46(11):5498-511.

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