Details of the Drug Formulation (DFM)

General Information of DFM (ID: F15237)
Name
Nifedipine 10 mg capsule
Company
Golden State Medical Supply
Active Pharmaceutical Ingredient (API) Nifedipine API Info click to show the detail info of this API
Angina pectoris ICD-11: BA40 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E09YYN DIG Info Eisenoxyd Colorant
E0IC9H DIG Info FD&C blue no. 1 Colorant
E06WYP DIG Info Glycerin Antimicrobial preservative ...
E04KSN DIG Info Hexahydric alcohol Diluent ...
E06CNF DIG Info Isobutyl alcohol Flavoring agent ...
E09ZXG DIG Info Menthol Flavoring agent
E05BSD DIG Info Titanium dioxide Coating agent ...
E0FU1S DIG Info Vinylpyrrolidone Binding agent ...
E0H2SC DIG Info Water Solvent
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM
      G-protein coupled receptor (GPCR)
            DBT Name: Serotonin receptor 2B (5HT2B) 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 FD&C blue no. 1
                    Biological Activity EC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID 5HT2B_HUMAN
            DBT Name: Cannabinoid CB2 receptor (CNR2) 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 FD&C blue no. 1
                    Biological Activity EC50 = 608.6 nM (estimated based on the structural similarity with CHEMBL2326294 ) [2]
                    Structural Similarity Tanimoto coefficient = 0.805970149
                    Tested Species Homo sapiens (Human)
                    UniProt ID CNR2_HUMAN
      Oxidoreductase (ORase)
            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 FD&C blue no. 1
                    Biological Activity IC50 = 22 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PGH2_HUMAN
      Hydrolase (HDase)
            DBT Name: Acetylcholinesterase (ACHE) 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 FD&C blue no. 1
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACES_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 FD&C blue no. 1
                    Biological Activity IC50 = 28 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID PDE4D_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 FD&C blue no. 1
                    Biological Activity Inhibition ratio = 80.5 % (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 FD&C blue no. 1
                    Biological Activity Ki = 13 uM (tested by experiment) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Transmembrane channel/porin (TC/P)
            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 Menthol
                    Biological Activity EC50 = 30000 nM (tested by experiment) [4]
                    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 Menthol
                    Biological Activity EC50 = 56000 nM (tested by experiment) [5]
                    Tested Species Mus musculus (Mouse)
                    UniProt ID TRPA1_MOUSE
            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 Menthol
                    Biological Activity EC50 = 3000 nM (tested by experiment) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID TRPM8_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Menthol
                    Biological Activity EC50 = 75000 nM (tested by experiment) [7]
                    Tested Species Rattus norvegicus (Rat)
                    UniProt ID TRPM8_RAT
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation. J Med Chem. 2013 Mar 14; 56(5):2045-58.
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 N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites. Eur J Med Chem. 2019 May 15; 170:141-156.
5 Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents. J Med Chem. 2010 Jul 22; 53(14):5085-107.
6 Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists. Bioorg Med Chem Lett. 2013 Nov 15; 23(22):6118-22.
7 Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators. J Med Chem. 2016 Mar 10; 59(5):2179-91.

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