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 | 141.26 | 28.45 | 53 | 2390 | 29104 | 50573577 |
Metastases to central nervous system | 95.03 | 28.45 | 31 | 2412 | 11251 | 50591430 |
Death | 78.69 | 28.45 | 87 | 2356 | 325292 | 50277389 |
Constipation | 71.39 | 28.45 | 64 | 2379 | 185644 | 50417037 |
Blood creatine phosphokinase increased | 59.97 | 28.45 | 28 | 2415 | 26339 | 50576342 |
Disease progression | 55.55 | 28.45 | 42 | 2401 | 95824 | 50506857 |
Pleural effusion | 50.10 | 28.45 | 37 | 2406 | 81417 | 50521264 |
Pneumonitis | 45.31 | 28.45 | 24 | 2419 | 29486 | 50573195 |
Interstitial lung disease | 39.22 | 28.45 | 27 | 2416 | 53149 | 50549532 |
Drug resistance | 33.61 | 28.45 | 17 | 2426 | 18972 | 50583709 |
Liver disorder | 32.50 | 28.45 | 21 | 2422 | 37201 | 50565480 |
Traumatic lung injury | 30.04 | 28.45 | 8 | 2435 | 1433 | 50601248 |
Hepatic function abnormal | 29.92 | 28.45 | 19 | 2424 | 32662 | 50570019 |
No adverse event | 29.45 | 28.45 | 19 | 2424 | 33559 | 50569122 |
Haemolysis | 29.29 | 28.45 | 11 | 2432 | 6005 | 50596676 |
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 | 79.00 | 35.16 | 93 | 1475 | 341991 | 29230968 |
Neoplasm progression | 73.69 | 35.16 | 30 | 1538 | 18582 | 29554377 |
Metastases to central nervous system | 55.91 | 35.16 | 19 | 1549 | 7112 | 29565847 |
Pneumonitis | 55.91 | 35.16 | 28 | 1540 | 28016 | 29544943 |
Interstitial lung disease | 53.68 | 35.16 | 35 | 1533 | 57683 | 29515276 |
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 | 132.35 | 30.39 | 56 | 3135 | 40908 | 64454633 |
Metastases to central nervous system | 107.34 | 30.39 | 36 | 3155 | 13876 | 64481665 |
Interstitial lung disease | 91.38 | 30.39 | 58 | 3133 | 97674 | 64397867 |
Death | 87.78 | 30.39 | 113 | 3078 | 482592 | 64012949 |
Pneumonitis | 76.55 | 30.39 | 41 | 3150 | 50324 | 64445217 |
Blood creatine phosphokinase increased | 73.44 | 30.39 | 42 | 3149 | 58516 | 64437025 |
Constipation | 67.43 | 30.39 | 69 | 3122 | 229268 | 64266273 |
Disease progression | 61.56 | 30.39 | 53 | 3138 | 141627 | 64353914 |
Pleural effusion | 54.26 | 30.39 | 47 | 3144 | 126512 | 64369029 |
Pericardial effusion | 46.11 | 30.39 | 27 | 3164 | 39227 | 64456314 |
Haemolysis | 45.51 | 30.39 | 18 | 3173 | 11021 | 64484520 |
Blood bilirubin increased | 38.95 | 30.39 | 28 | 3163 | 57525 | 64438016 |
Liver disorder | 38.52 | 30.39 | 27 | 3164 | 53324 | 64442217 |
Traumatic lung injury | 34.99 | 30.39 | 10 | 3181 | 2266 | 64493275 |
Hepatic function abnormal | 34.01 | 30.39 | 27 | 3164 | 64286 | 64431255 |
Bradycardia | 33.60 | 30.39 | 35 | 3156 | 118184 | 64377357 |
Blood creatinine increased | 32.99 | 30.39 | 37 | 3154 | 135745 | 64359796 |
Hyperbilirubinaemia | 31.44 | 30.39 | 17 | 3174 | 21188 | 64474353 |
None
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 | antineoplastic agents |
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 |
None
None
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 |
4035251 | VANDF |
CHEBI:90936 | CHEBI |
EMH | PDB_CHEM_ID |
CHEMBL1738797 | ChEMBL_ID |
C582670 | MESH_SUPPLEMENTAL_RECORD_UI |
7739 | IUPHAR_LIGAND_ID |
9699 | INN_ID |
1256589-74-8 | SECONDARY_CAS_RN |
DB11363 | DRUGBANK_ID |
LIJ4CT1Z3Y | UNII |
49806720 | PUBCHEM_CID |
1727454 | RXNORM |
237548 | MMSL |
31372 | MMSL |
d08405 | MMSL |
716039000 | SNOMEDCT_US |
716040003 | SNOMEDCT_US |
781316007 | SNOMEDCT_US |
C3853921 | UMLSCUI |
CHEMBL3707320 | ChEMBL_ID |
016628 | NDDF |
016629 | NDDF |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
ALECENSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50242-130 | CAPSULE | 150 mg | ORAL | NDA | 29 sections |
ALECENSA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50242-130 | CAPSULE | 150 mg | ORAL | NDA | 29 sections |