Details of the Drug Formulation (DFM)

General Information of DFM (ID: F03818)
Name
Cephalexin 250 mg capsule
Company
Pharma-C
Active Pharmaceutical Ingredient (API) Cephalexin API Info click to show the detail info of this API
Acute otitis media ICD-11: AB00 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0A1CS DIG Info Ammonia Alkalizing agent
E0SJ4H DIG Info Beta-D-lactose Diluent ...
E01VDF DIG Info Butyl alcohol Flavoring agent ...
E0IC9H DIG Info FD&C blue no. 1 Colorant
E02FBG DIG Info Ferrosoferric oxide Colorant
E08XEK DIG Info Hydrazine yellow Colorant
E0N2PK DIG Info Isopropyl alcohol Antimicrobial preservative ...
E01UTP DIG Info Magnesium stearate lubricant
E0ND5Z DIG Info Potassium hydroxide Alkalizing agent
E0M1JK DIG Info Propylene glycol Antimicrobial preservative ...
E01UTV DIG Info Silicon dioxide Anticaking agent ...
E0QY1F DIG Info Talc Anticaking agent ...
E05BSD DIG Info Titanium dioxide Coating 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
            DBT Name: Opioid receptor mu (OPRM1) 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 Hydrazine yellow
                    Biological Activity IC50 = 16 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID OPRM_HUMAN
            DBT Name: Dopamine D1 receptor (DRD1) 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 Hydrazine yellow
                    Biological Activity IC50 = 23 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD1_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
            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) [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 Magnesium stearate
                    Biological Activity Protein expression downregulation (tested by experiment) [4]
                    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 Silicon dioxide
                    Biological Activity Protein expression downregulation (tested by experiment) [4]
                    Tested Species Homo sapiens (Human)
                    UniProt ID CP3A4_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: Tyrosyl-DNA phosphodiesterase 2 (TDP2) 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 Hydrazine yellow
                    Biological Activity IC50 = 3500 nM (estimated based on the structural similarity with CHEMBL3813826 ) [5]
                    Structural Similarity Tanimoto coefficient = 0.777777778
                    Tested Species Homo sapiens (Human)
                    UniProt ID TYDP2_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) [6]
                    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) [6]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SO2B1_HUMAN
      Transmembrane channel/porin (TC/P)
            DBT Name: GABA(A) receptor alpha-1 (GABRA1) 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 Hydrazine yellow
                    Biological Activity IC50 = 13 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID GBRA1_HUMAN
      Cell line (CELL)
            DBT Name: Lymphoma P388/ADR cells (P388/ADR) 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 Isopropyl alcohol
                    Biological Activity IC50 = 0.22 uM (estimated based on the structural similarity with CHEMBL545 ) [7]
                    Structural Similarity Tanimoto coefficient = 0.789473684
                    Tested Species Mus musculus (Mouse)
                    Cellosaurus ID CVCL_IZ75
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 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
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 Discovery of selective inhibitors of tyrosyl-DNA phosphodiesterase 2 by targeting the enzyme DNA-binding cleft. Bioorg Med Chem Lett. 2016 Jul 15; 26(14):3232-3236.
6 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.
7 Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11; 47(6):1413-22.

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