Details of the Drug Formulation (DFM)

General Information of DFM (ID: F04454)
Name
Clarithromycin 500 mg tablet
Company
Actavis Pharma; AvKARE; PD-Rx Pharmaceuticals
Active Pharmaceutical Ingredient (API) Clarithromycin API Info click to show the detail info of this API
Pneumocystis pneumonia ICD-11: CA40 Approved
Drug Inactive Ingredient (DIGs)
DIG ID DIG Info DIG Name DIG Functional Class
E0H2RX DIG Info Glyceryl monostearate Emollient ...
E0H6BT DIG Info Quinoline yellow WS Colorant
E0Q3PU DIG Info Saccharose Binding agent ...
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
      G-protein coupled receptor (GPCR)
            DBT Name: Alpha-2A adrenoceptor (ADA2A) 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 Quinoline yellow WS
                    Biological Activity IC50 = 28 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ADA2A_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 Quinoline yellow WS
                    Biological Activity IC50 = 26 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID DRD3_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 Quinoline yellow WS
                    Biological Activity IC50 > 10 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ACES_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) [2]
                    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) [3]
                    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) [3]
                    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) [3]
                    Tested Species Homo sapiens (Human)
                    UniProt ID MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN
      Potential-driven transporter (PDT)
            DBT Name: Dopamine transporter (DAT) 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 Quinoline yellow WS
                    Biological Activity IC50 = 29 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID SC6A3_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 (1) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity EC50 = 13156.33 nM (estimated based on the structural similarity with CHEMBL1417293 ) [4]
                    Structural Similarity Tanimoto coefficient = 0.828729282
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
               Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT
                    Interacting DIG Quinoline yellow WS
                    Biological Activity IC50 = 18 uM (tested by experiment) [1]
                    Tested Species Homo sapiens (Human)
                    UniProt ID ESR1_HUMAN
      Cell line (CELL)
            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) [5]
                    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 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.
3 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.
4 PubChem BioAssay data set.
5 Lignanamides and nonalkaloidal components of Hyoscyamus niger seeds. J Nat Prod. 2002 Feb; 65(2):206-9.

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