Details of the Drug Formulation (DFM)
General Information of DFM (ID: F05058) | |||||
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Name |
Crofelemer 125 mg tablet
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Company |
Napo Pharmaceuticals
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Active Pharmaceutical Ingredient (API) | Crofelemer | API Info click to show the detail info of this API | |||
Human immunodeficiency virus infection | ICD-11: 1C60 | Approved | |||
Drug Inactive Ingredient (DIGs) | |||||
DIG ID | DIG Info | DIG Name | DIG Functional Class | ||
E03SQI | DIG Info | Carmellose sodium | Disintegrant | ||
E0MF5O | DIG Info | Ethyl acrylate | Film/membrane-forming agent ... | ||
E01UTP | DIG Info | Magnesium stearate | lubricant | ||
E0V6QI | DIG Info | methylparaben | Antimicrobial preservative | ||
E0KP0P | DIG Info | Propyl 4-hydroxybenzoate | Antimicrobial preservative | ||
E01UTV | DIG Info | Silicon dioxide | Anticaking agent ... | ||
E0QY1F | DIG Info | Talc | Anticaking agent ... | ||
E05BSD | DIG Info | Titanium dioxide | Coating agent ... | ||
E0K0OU | DIG Info | Triethyl citrate | Plasticizing agent ... | ||
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: Muscarinic receptor M1 (ACM1) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 = 23 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | ACM1_HUMAN | |||||
Oxidoreductase (ORase) | ||||||
DBT Name: Prostaglandin G/H synthase 1 (COX-1) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 > 3 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | PGH1_HUMAN | |||||
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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 > 3 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 | 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 | Carmellose sodium | |||||
Biological Activity | Protein expression upregulation (tested by experiment) | [2] | ||||
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 | Carmellose sodium | |||||
Biological Activity | Protein expression upregulation (tested by experiment) | [2] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP3A4_HUMAN | |||||
Experiment (4) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | Silicon dioxide | |||||
Biological Activity | Protein expression downregulation (tested by experiment) | [2] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CP3A4_HUMAN | |||||
Transferase (TFase) | ||||||
DBT Name: VEGF-2 receptor (KDR) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 = 24 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | VGFR2_HUMAN | |||||
Hydrolase (HDase) | ||||||
DBT Name: Leukotriene A-4 hydrolase (LTA4H) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | Ki = 260 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | LKHA4_HUMAN | |||||
Lyase/isomerase/ligase (L/I/G) | ||||||
DBT Name: Carbonic anhydrase I (CA1) | 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 | methylparaben | |||||
Biological Activity | Ki = 2600 nM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH1_HUMAN | |||||
DBT Name: Carbonic anhydrase II (CA2) | 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 | methylparaben | |||||
Biological Activity | Ki = 3400 nM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH2_HUMAN | |||||
DBT Name: Carbonic anhydrase IX (CA9) | 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 | methylparaben | |||||
Biological Activity | Ki = 5500 nM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH9_HUMAN | |||||
DBT Name: Carbonic anhydrase VII (CA7) | 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 | methylparaben | |||||
Biological Activity | Ki = 780 nM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH7_HUMAN | |||||
DBT Name: Carbonic anhydrase XII (CA12) | 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 | methylparaben | |||||
Biological Activity | Ki = 820 nM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH12_HUMAN | |||||
DBT Name: Carbonic anhydrase XIV (CA14) | 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 | methylparaben | |||||
Biological Activity | Ki = 4100 nM (tested by experiment) | [3] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | CAH14_HUMAN | |||||
Potential-driven transporter (PDT) | ||||||
DBT Name: Norepinephrine transporter (NET) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 = 30 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SC6A2_HUMAN | |||||
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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | Inhibition ratio = 25.1 % (tested by experiment) | [4] | ||||
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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | Ki = 200 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | SO2B1_HUMAN | |||||
Nuclear receptor (NR) | ||||||
DBT Name: Androgen receptor (AR) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 = 309029.54 nM (tested by experiment) | [5] | ||||
Tested Species | Rattus norvegicus (Rat) | |||||
UniProt ID | ANDR_RAT | |||||
Experiment (2) for Assessing the Biological Activity of the Studied DIG on This DBT | ||||||
Interacting DIG | methylparaben | |||||
Biological Activity | IC50 > 426579.52 nM (tested by experiment) | [5] | ||||
Tested Species | Rattus norvegicus (Rat) | |||||
UniProt ID | ANDR_RAT | |||||
DBT Name: Estrogen receptor alpha (ESR1) | 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 | Propyl 4-hydroxybenzoate | |||||
Biological Activity | IC50 = 11 uM (tested by experiment) | [1] | ||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | ESR1_HUMAN | |||||
Other protein families (OPF) | ||||||
DBT Name: NFE2-related factor 2 (NRF2) | 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 | Ethyl acrylate | |||||
Biological Activity | EC50 = 5110 nM (estimated based on the structural similarity with CHEMBL2107333 ) | [6] | ||||
Structural Similarity | Tanimoto coefficient = 0.837837838 | |||||
Tested Species | Homo sapiens (Human) | |||||
UniProt ID | NF2L2_HUMAN | |||||
Cell line (CELL) | ||||||
DBT Name: Lung cancer A-549 cells (A-549) | 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 | methylparaben | |||||
Biological Activity | IC50 > 20 ug.mL-1 (tested by experiment) | [7] | ||||
Tested Species | Homo sapiens (Human) | |||||
Cellosaurus ID | CVCL_0023 | |||||
DBT Name: Hepatoblastoma HepG2 cells (HepG2) | 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 | methylparaben | |||||
Biological Activity | IC50 > 20 ug.mL-1 (tested by experiment) | [7] | ||||
Tested Species | Homo sapiens (Human) | |||||
Cellosaurus ID | CVCL_0027 | |||||
DBT Name: Cervical cancer KB cells (KB) | 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 | methylparaben | |||||
Biological Activity | IC50 > 200000 nM (tested by experiment) | [8] | ||||
Tested Species | Homo sapiens (Human) | |||||
Cellosaurus ID | CVCL_0372 | |||||
DBT Name: Carcinoma MDA-MB-231 cells (MDA-MB-231) | 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 | methylparaben | |||||
Biological Activity | IC50 > 20 ug.mL-1 (tested by experiment) | [7] | ||||
Tested Species | Homo sapiens (Human) | |||||
Cellosaurus ID | CVCL_0062 | |||||
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