Details of the Drug Formulation (DFM)
General Information of DFM (ID: F23352) | |||||
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Name |
Niraparib Tosylate 100mg capsule
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Company |
Glaxosmithkline
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Active Pharmaceutical Ingredient (API) | Niraparib | API Info click to show the detail info of this API | |||
Ovarian cancer | ICD-11: 2C73 | Approved | |||
Drug Inactive Ingredient (DIGs) | |||||
DIG ID | DIG Info | DIG Name | DIG Functional Class | ||
E0A1CS | DIG Info | Ammonia | Alkalizing agent | ||
E01VDF | DIG Info | Butyl alcohol | Flavoring agent ... | ||
E05PRI | DIG Info | Erythrosine sodium anhydrous | Colorant | ||
E0SF4Y | DIG Info | Ethanol | Antimicrobial preservative ... | ||
E0IC9H | DIG Info | FD&C blue no. 1 | Colorant | ||
E0U4QR | DIG Info | FD&C yellow no. 5 free acid | Colorant | ||
E0T2WF | DIG Info | Ferric oxide black | Colorant | ||
E00FTX | DIG Info | Gelatin | Other agent | ||
E0N2PK | DIG Info | Isopropyl alcohol | Antimicrobial preservative ... | ||
E00DHW | DIG Info | Lactose monohydrate | Binding agent ... | ||
E01UTP | DIG Info | Magnesium stearate | lubricant | ||
E0ND5Z | DIG Info | Potassium hydroxide | Alkalizing agent | ||
E0M1JK | DIG Info | Propylene glycol | Antimicrobial preservative ... | ||
E0WM1T | DIG Info | Shellac | Coating 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 | ||||||
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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 | |||||
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 | |||||
DBT Name: Cytochrome P450 2E1 (CYP2E1) | 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 | Gelatin | |||||
Biological Activity | IC50 = 141.2 uM (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2E1_HUMAN | |||||
DBT Name: Cytochrome P450 2C9 (CYP2C9) | 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 | Gelatin | |||||
Biological Activity | EC50 = 249.5 uM (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2C9_HUMAN | |||||
DBT Name: Mephenytoin 4-hydroxylase (CYP2C19) | 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 | Gelatin | |||||
Biological Activity | EC50 = 20.5 uM (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2CJ_HUMAN | |||||
DBT Name: Debrisoquine 4-hydroxylase (CYP2D6) | 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 | Gelatin | |||||
Biological Activity | EC50 = 379.9 uM (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP2D6_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: Caspase-3 (CASP3) | 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 yellow no. 5 free acid | |||||
Biological Activity | IC50 = 100000 nM (estimated based on the structural similarity with CHEMBL3145148 ) | [6] | ||||
Structural Similarity | Tanimoto coefficient = 0.797101449 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CASP3_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 | |||||
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 | Gelatin | |||||
Biological Activity | IC50 = 40.9 uM (tested by experiment) | [5] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP1A2_HUMAN | |||||
Primary active transporter (PAT) | ||||||
DBT Name: Multidrug resistance protein 3 (ABCC3) | 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 | Erythrosine sodium anhydrous | |||||
Biological Activity | IC50 = 133000 nM (estimated based on the structural similarity with CHEMBL177756 ) | [7] | ||||
Structural Similarity | Tanimoto coefficient = 0.90070922 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | MRP3_HUMAN | |||||
DBT Name: Multidrug resistance protein 4 (ABCC4) | 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 | Erythrosine sodium anhydrous | |||||
Biological Activity | IC50 = 133000 nM (estimated based on the structural similarity with CHEMBL177756 ) | [7] | ||||
Structural Similarity | Tanimoto coefficient = 0.90070922 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | MRP4_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) | [8] | ||||
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) | [8] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_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 ) | [9] | ||||
Structural Similarity | Tanimoto coefficient = 0.789473684 | |||||
Tested Species | Mus musculus (Mouse) | |||||
Cellosaurus ID | CVCL_IZ75 | |||||
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