Details of the Drug Formulation (DFM)
General Information of DFM (ID: F18229) | |||||
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Name |
Protriptyline 5 mg tablet
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Company |
Epic Pharma; Hi-Tech Pharmacal
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Active Pharmaceutical Ingredient (API) | Protriptyline |
API Info
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Major depressive disorder | ICD-11: 6A70 | Approved | |||
Drug Inactive Ingredient (DIGs) | |||||
DIG ID | DIG Info | DIG Name | DIG Functional Class | ||
E00DHW | DIG Info | Lactose monohydrate | Binding agent ... | ||
E01UTP | DIG Info | Magnesium stearate | lubricant | ||
E0AQ3D | DIG Info | Polysorbate 20 | Dispersing agent ... | ||
E0L0MR | DIG Info | Sunset yellow FCF | Colorant | ||
E05BSD | DIG Info | Titanium dioxide | Coating agent ... | ||
E0T2AJ | DIG Info | Triacetin | Humectant ... | ||
Full List of Biological Targets of DIG (DBTs) Regulated by DIG(s) in This DFM | ||||||
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Oxidoreductase (ORase) | ||||||
DBT Name: Cytochrome P450 3A (CYP3A) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | IC50 = 320 uM (tested by experiment) | [1] | ||||
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
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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) | [2] | ||||
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 20 | |||||
Biological Activity | EC50 = 363.7 uM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP3A4_HUMAN | |||||
DBT Name: Cytochrome P450 2E1 (CYP2E1) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | IC50 = 64.1 uM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2E1_HUMAN | |||||
DBT Name: Cytochrome P450 2C9 (CYP2C9) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | EC50 = 228.4 uM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2C9_HUMAN | |||||
DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | IC50 = 230 uM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2CJ_HUMAN | |||||
DBT Name: Cytochrome P450 3A5 (CYP3A5) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | IC50 = 84 uM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP3A5_HUMAN | |||||
Primary active transporter (PAT) | ||||||
DBT Name: Multidrug resistance protein 1 (ABCB1) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | IC50 = 0.25 mg.mL-1 (tested by experiment) | [4] | ||||
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 | Polysorbate 20 | |||||
Biological Activity | Inhibition ratio > 240 % (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | MDR1_HUMAN ; MDR3_HUMAN ; ABCB5_HUMAN | |||||
DBT Name: Urate exporter (BCRP) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | Inhibition ratio > 84 % (tested by experiment) | [6] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | ABCG2_HUMAN | |||||
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Polysorbate 20 | |||||
Biological Activity | Inhibition ratio > 50 % (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | ABCG2_HUMAN | |||||
Potential-driven transporter (PDT) | ||||||
DBT Name: Solute carrier SLCO2B1 (OATPB) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment (1) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Sunset yellow FCF | |||||
Biological Activity | Inhibition ratio = 54.5 % (tested by experiment) | [7] | ||||
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 | Sunset yellow FCF | |||||
Biological Activity | Ki = 68.4 uM (tested by experiment) | [7] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Experiment (3) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Sunset yellow FCF | |||||
Biological Activity | Ki = 74 uM (tested by experiment) | [8] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Other protein families (OPF) | ||||||
DBT Name: Thrombopoietin receptor (MPL) | Click to Show/Hide | |||||
Detailed Information |
DBT Info
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Experiment for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Sunset yellow FCF | |||||
Biological Activity | EC50 = 3000 nM (estimated based on the structural similarity with CHEMBL122867 ) | [9] | ||||
Structural Similarity | Tanimoto coefficient = 0.93081761 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | TPOR_HUMAN | |||||
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