Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4866 | 1032900-25-6 |
None
None
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 26, 2015 | EMA | ||
April 29, 2014 | FDA | NOVARTIS PHARMS CORP |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Malignant neoplasm progression | 418.43 | 32.95 | 150 | 2419 | 64776 | 46618717 |
Non-small cell lung cancer stage IV | 265.43 | 32.95 | 38 | 2531 | 199 | 46683294 |
Non-small cell lung cancer | 228.31 | 32.95 | 49 | 2520 | 3095 | 46680398 |
Metastases to central nervous system | 225.13 | 32.95 | 62 | 2507 | 11159 | 46672334 |
Diarrhoea | 116.28 | 32.95 | 147 | 2422 | 559455 | 46124038 |
Nausea | 80.44 | 32.95 | 138 | 2431 | 687316 | 45996177 |
Vomiting | 72.23 | 32.95 | 105 | 2464 | 452689 | 46230804 |
Death | 49.22 | 32.95 | 75 | 2494 | 335473 | 46348020 |
Lung adenocarcinoma | 43.71 | 32.95 | 14 | 2555 | 4190 | 46679303 |
Pericarditis | 41.35 | 32.95 | 22 | 2547 | 23905 | 46659588 |
Pericardial effusion | 40.00 | 32.95 | 22 | 2547 | 25521 | 46657972 |
Alanine aminotransferase increased | 39.09 | 32.95 | 35 | 2534 | 88416 | 46595077 |
Neoplasm progression | 36.41 | 32.95 | 21 | 2548 | 26662 | 46656831 |
Decreased appetite | 35.14 | 32.95 | 48 | 2521 | 193788 | 46489705 |
Lung neoplasm malignant | 34.78 | 32.95 | 17 | 2552 | 15472 | 46668021 |
Aspartate aminotransferase increased | 34.49 | 32.95 | 31 | 2538 | 78669 | 46604824 |
Hyperglycaemia | 33.55 | 32.95 | 22 | 2547 | 35049 | 46648444 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Malignant neoplasm progression | 329.32 | 38.95 | 130 | 1555 | 72157 | 29878636 |
Non-small cell lung cancer | 235.67 | 38.95 | 52 | 1633 | 3678 | 29947115 |
Metastases to central nervous system | 148.74 | 38.95 | 41 | 1644 | 7243 | 29943550 |
Non-small cell lung cancer stage IV | 121.58 | 38.95 | 19 | 1666 | 189 | 29950604 |
Diarrhoea | 61.85 | 38.95 | 84 | 1601 | 334019 | 29616774 |
Nausea | 49.33 | 38.95 | 71 | 1614 | 296886 | 29653907 |
Pericarditis | 47.66 | 38.95 | 18 | 1667 | 8588 | 29942205 |
Lung neoplasm malignant | 44.10 | 38.95 | 20 | 1665 | 15112 | 29935681 |
Metastases to liver | 41.92 | 38.95 | 18 | 1667 | 11947 | 29938846 |
Source | Code | Description |
---|---|---|
ATC | L01ED02 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Anaplastic lymphoma kinase (ALK) inhibitors |
FDA MoA | N0000020001 | Tyrosine Kinase Inhibitors |
FDA EPC | N0000175605 | Kinase Inhibitor |
MeSH PA | D000970 | Antineoplastic Agents |
MeSH PA | D004791 | Enzyme Inhibitors |
MeSH PA | D047428 | Protein Kinase Inhibitors |
FDA MoA | N0000185504 | Cytochrome P450 2C9 Inhibitors |
FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
CHEBI has role | CHEBI:35610 | cytostatic |
CHEBI has role | CHEBI:62434 | alk inhibitor |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Non-small cell lung cancer | indication | 254637007 | DOID:3908 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 10.21 | Basic |
pKa2 | 2.49 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
150MG | ZYKADIA | NOVARTIS | N205755 | April 29, 2014 | DISCN | CAPSULE | ORAL | April 29, 2021 | TREATMENT OF PATIENTS WITH ANULLPLASTIC LYMPHOMA KINULLSE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB. |
150MG | ZYKADIA | NOVARTIS | N211225 | March 18, 2019 | RX | TABLET | ORAL | April 29, 2021 | FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S) |
150MG | ZYKADIA | NOVARTIS | N205755 | April 29, 2014 | DISCN | CAPSULE | ORAL | May 26, 2024 | TREATMENT OF PATIENTS WITH METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC) WHOSE TUMORS ARE ANULLPLASTIC LYMPHOMA KINULLSE (ALK)-POSITIVE AS DETECTED BY AN FDA-APPROVED TEST |
150MG | ZYKADIA | NOVARTIS | N211225 | March 18, 2019 | RX | TABLET | ORAL | May 26, 2024 | FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S) |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
ALK tyrosine kinase receptor | Kinase | INHIBITOR | IC50 | 9.70 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
Insulin receptor | Kinase | AGONIST | IC50 | 8.15 | SCIENTIFIC LITERATURE | ||||
Testis-specific serine/threonine-protein kinase 1 | Kinase | IC50 | 7.64 | SCIENTIFIC LITERATURE | |||||
Fibroblast growth factor receptor 2 | Kinase | IC50 | 6.59 | CHEMBL | |||||
Tyrosine-protein kinase ABL1 | Kinase | IC50 | 5.90 | CHEMBL | |||||
Receptor-type tyrosine-protein kinase FLT3 | Kinase | IC50 | 7.22 | CHEMBL | |||||
Epidermal growth factor receptor | Kinase | IC50 | 6.05 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase Src | Kinase | IC50 | 5.77 | CHEMBL | |||||
Vascular endothelial growth factor receptor 2 | Kinase | IC50 | 5.38 | CHEMBL | |||||
Fibroblast growth factor receptor 3 | Kinase | IC50 | 6.37 | CHEMBL | |||||
Fibroblast growth factor receptor 4 | Kinase | IC50 | 6.02 | CHEMBL | |||||
Platelet-derived growth factor receptor alpha | Kinase | IC50 | 5.94 | CHEMBL | |||||
Hepatocyte growth factor receptor | Kinase | IC50 | 5.87 | CHEMBL | |||||
Tyrosine-protein kinase JAK2 | Kinase | IC50 | 6.21 | CHEMBL | |||||
Tyrosine-protein kinase JAK1 | Kinase | IC50 | 5.43 | CHEMBL | |||||
Tyrosine-protein kinase SYK | Kinase | IC50 | 5.52 | CHEMBL | |||||
Tyrosine-protein kinase BTK | Kinase | IC50 | 5.47 | CHEMBL | |||||
Tyrosine-protein kinase Fgr | Kinase | IC50 | 5.71 | CHEMBL | |||||
Tyrosine-protein kinase JAK3 | Kinase | IC50 | 5.10 | CHEMBL | |||||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.90 | CHEMBL | |||||
High affinity nerve growth factor receptor | Kinase | IC50 | 5.56 | CHEMBL | |||||
Mast/stem cell growth factor receptor Kit | Kinase | IC50 | 5.89 | CHEMBL | |||||
MAP kinase-interacting serine/threonine-protein kinase 2 | Kinase | IC50 | 5.65 | CHEMBL | |||||
Tyrosine-protein kinase Lyn | Kinase | IC50 | 6.08 | CHEMBL | |||||
Tyrosine-protein kinase ZAP-70 | Kinase | IC50 | 5.01 | CHEMBL | |||||
Cyclin-dependent kinase 2 | Kinase | IC50 | 5.40 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase ROS | Kinase | IC50 | 6.85 | CHEMBL | |||||
Rho-associated protein kinase 2 | Kinase | IC50 | 5.90 | CHEMBL | |||||
Transcription factor ETV6 | Transcription factor | IC50 | 5.49 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | IC50 | 6.40 | CHEMBL | |||||
Tyrosine-protein kinase Lck | Kinase | IC50 | 6.25 | CHEMBL | |||||
BDNF/NT-3 growth factors receptor | Kinase | IC50 | 5.74 | CHEMBL | |||||
Insulin-like growth factor 1 receptor | Kinase | IC50 | 8.10 | SCIENTIFIC LITERATURE | |||||
Cyclin-dependent kinase 4 | Kinase | IC50 | 5.33 | CHEMBL |
ID | Source |
---|---|
D10551 | KEGG_DRUG |
4033301 | VUID |
N0000190753 | NUI |
4033301 | VANDF |
C3818721 | UMLSCUI |
CHEBI:78432 | CHEBI |
4MK | PDB_CHEM_ID |
CHEMBL2403108 | ChEMBL_ID |
DB09063 | DRUGBANK_ID |
C586847 | MESH_SUPPLEMENTAL_RECORD_UI |
57379345 | PUBCHEM_CID |
7397 | IUPHAR_LIGAND_ID |
9817 | INN_ID |
K418KG2GET | UNII |
1535457 | RXNORM |
219616 | MMSL |
30281 | MMSL |
d08255 | MMSL |
015504 | NDDF |
703146007 | SNOMEDCT_US |
704310000 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
ZYKADIA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0640 | CAPSULE | 150 mg | ORAL | NDA | 28 sections |
ZYKADIA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-0694 | TABLET, FILM COATED | 150 mg | ORAL | NDA | 28 sections |