Stem definition | Drug id | CAS RN |
---|---|---|
tyrosine kinase inhibitors | 4937 | 1256580-46-7 |
Dose | Unit | Route |
---|---|---|
1.20 | g | O |
Property | Value | Reference |
---|---|---|
Vd (Volume of distribution) | 6.35 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 7.69 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 11.70 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Feb. 16, 2017 | EMA | Roche Registration Limited | |
Dec. 11, 2015 | FDA | HOFFMAN-LA ROCHE | |
July 4, 2014 | PMDA | Chugai Pharmaceutical Co., Ltd |
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 |
---|---|---|---|---|---|---|
Neoplasm progression | 140.18 | 28.03 | 52 | 2335 | 29867 | 53316812 |
Metastases to central nervous system | 95.32 | 28.03 | 31 | 2356 | 12026 | 53334653 |
Death | 74.04 | 28.03 | 85 | 2302 | 357147 | 52989532 |
Constipation | 71.94 | 28.03 | 64 | 2323 | 198348 | 53148331 |
Blood creatine phosphokinase increased | 56.41 | 28.03 | 27 | 2360 | 28958 | 53317721 |
Pleural effusion | 49.85 | 28.03 | 37 | 2350 | 88542 | 53258137 |
Pneumonitis | 43.16 | 28.03 | 23 | 2364 | 30865 | 53315814 |
Disease progression | 41.09 | 28.03 | 35 | 2352 | 101885 | 53244794 |
Interstitial lung disease | 38.70 | 28.03 | 27 | 2360 | 58595 | 53288084 |
Drug resistance | 31.11 | 28.03 | 16 | 2371 | 19946 | 53326733 |
Traumatic lung injury | 30.21 | 28.03 | 8 | 2379 | 1515 | 53345164 |
Liver disorder | 30.06 | 28.03 | 20 | 2367 | 40135 | 53306544 |
No adverse event | 28.06 | 28.03 | 19 | 2368 | 39246 | 53307433 |
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 |
---|---|---|---|---|---|---|
Death | 73.18 | 37.01 | 89 | 1436 | 382428 | 32129573 |
Neoplasm progression | 72.19 | 37.01 | 29 | 1496 | 19629 | 32492372 |
Pneumonitis | 54.28 | 37.01 | 27 | 1498 | 30107 | 32481894 |
Metastases to central nervous system | 52.80 | 37.01 | 18 | 1507 | 7690 | 32504311 |
Interstitial lung disease | 44.20 | 37.01 | 31 | 1494 | 64970 | 32447031 |
Source | Code | Description |
---|---|---|
ATC | L01ED03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Anaplastic lymphoma kinase (ALK) inhibitors |
FDA MoA | N0000175082 | Kinase Inhibitors |
FDA EPC | N0000175605 | Kinase Inhibitor |
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 |
Anaplastic lymphoma kinase positive anaplastic large cell lymphoma | indication | 738770003 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.42 | acidic |
pKa2 | 7.47 | Basic |
pKa3 | 4.89 | Basic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
EQ 150MG BASE | ALECENSA | HOFFMANN-LA ROCHE | N208434 | Dec. 11, 2015 | RX | CAPSULE | ORAL | Dec. 11, 2022 | TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK)-POSITIVE METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB |
EQ 150MG BASE | ALECENSA | HOFFMANN-LA ROCHE | N208434 | Dec. 11, 2015 | RX | CAPSULE | ORAL | Nov. 6, 2024 | FOR TREATMENT OF PATIENTS WITH ANAPLASTIC LYMPHOMA KINASE (ALK) POSITIVE, METASTATIC NON-SMALL-CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST, EXCLUDING PATIENTS WHO HAVE PROGRESSED ON OR ARE INTOLERANT TO CRIZOTINIB |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
ALK tyrosine kinase receptor | Kinase | INHIBITOR | IC50 | 8.72 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | INHIBITOR | IC50 | 8.32 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
Tyrosine-protein kinase Fer | Kinase | Kd | 5.42 | CHEMBL | |||||
Dual specificity protein kinase CLK1 | Kinase | Kd | 4.53 | CHEMBL | |||||
Dual specificity protein kinase CLK2 | Kinase | Kd | 5.63 | CHEMBL | |||||
Dual specificity protein kinase CLK3 | Kinase | Kd | 5.86 | CHEMBL | |||||
Cyclin-G-associated kinase | Kinase | Kd | 6.59 | CHEMBL | |||||
Calcium/calmodulin-dependent protein kinase kinase 2 | Kinase | Kd | 4.45 | CHEMBL | |||||
Vascular endothelial growth factor receptor 2 | Kinase | IC50 | 5.85 | CHEMBL | |||||
SRSF protein kinase 1 | Kinase | IC50 | 6.71 | CHEMBL | |||||
Ephrin type-A receptor 1 | Kinase | Kd | 6.71 | CHEMBL | |||||
Proto-oncogene tyrosine-protein kinase ROS | Kinase | Ki | 5.70 | CHEMBL | |||||
Peroxisomal acyl-coenzyme A oxidase 3 | Enzyme | Kd | 5.58 | CHEMBL | |||||
Peroxisomal acyl-coenzyme A oxidase 1 | Enzyme | Kd | 6.57 | CHEMBL | |||||
Casein kinase I isoform gamma-2 | Kinase | Kd | 6.29 | CHEMBL | |||||
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Kinase | Kd | 5.77 | CHEMBL |
ID | Source |
---|---|
D10450 | KEGG_DRUG |
1256589-74-8 | SECONDARY_CAS_RN |
4035251 | VANDF |
CHEBI:90936 | CHEBI |
EMH | PDB_CHEM_ID |
CHEMBL1738797 | ChEMBL_ID |
C582670 | MESH_SUPPLEMENTAL_RECORD_UI |
7739 | IUPHAR_LIGAND_ID |
9699 | INN_ID |
DB11363 | DRUGBANK_ID |
LIJ4CT1Z3Y | UNII |
49806720 | PUBCHEM_CID |
1727454 | RXNORM |
237548 | MMSL |
31372 | MMSL |
d08405 | MMSL |
016628 | NDDF |
016629 | NDDF |
716039000 | SNOMEDCT_US |
716040003 | SNOMEDCT_US |
781316007 | SNOMEDCT_US |
C3853921 | UMLSCUI |
CHEMBL3707320 | ChEMBL_ID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
ALECENSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50242-130 | CAPSULE | 150 mg | ORAL | NDA | 29 sections |