Crizotinib

CAS 877399-52-5

Crizotinib (CAS 877399-52-5) is a pharmaceutical compound with 80 bioactivity targets and 674 adverse event associations.

SOURCE NLM DailyMed
Label records
0
SOURCE EMBL-EBI ChEMBL
Bioactivity
158
SOURCE DrugCentral
Adverse signals
674
SOURCE IUPHAR/BPS
PubMed IDs
3
SOURCE DrugCentral 055904D152D6

Compound Identity

Matched identifiers and naming fields for the pharmaceutical compound record.

Primary Name
Crizotinib
CAS Number
877399-52-5
UNII
53AH36668S
InChIKey
KTEIFNKAUNYNJU-GFCCVEGCSA-N
ChEMBL ID
CHEMBL601719
DrugCentral Struct ID
4187
Source Match
DrugCentral (CAS), FDA GSRS (UNII)
Synonyms and normalized names
Xalkori
SOURCE EMBL-EBI ChEMBL 80 bioactivity rows

Bioactivity & Target Interactions

Target-level activity records with assay counts, activity type, and measured value where present.

TargetActivity ValueAssaysOrganism
Tyrosine-protein kinase JAK3
Kinase
Kd 6.7 - Homo sapiens
Macrophage-stimulating protein receptor
Kinase
Kd 7.6 - Homo sapiens
Tyrosine-protein kinase ABL1
Kinase
Kd 8 - Homo sapiens
Mast/stem cell growth factor receptor Kit
Kinase
Kd 6.1 - Homo sapiens
Epidermal growth factor receptor
Kinase
Kd 5.57 - Homo sapiens
Breakpoint cluster region protein
Kinase
Kd 5.61 - Homo sapiens
Proto-oncogene tyrosine-protein kinase Src
Kinase
Kd 6.25 - Homo sapiens
Tyrosine-protein kinase Lck
Kinase
Kd 7.52 - Homo sapiens
Tyrosine-protein kinase Yes
Kinase
Kd 6.11 - Homo sapiens
Tyrosine-protein kinase Fyn
Kinase
Kd 5.89 - Homo sapiens
Ephrin type-A receptor 2
Kinase
Kd 7 - Homo sapiens
Receptor-type tyrosine-protein kinase FLT3
Kinase
Kd 6.68 - Homo sapiens
Proto-oncogene tyrosine-protein kinase receptor Ret
Kinase
Kd 5.89 - Homo sapiens
Vascular endothelial growth factor receptor 1
Kinase
Kd 5.64 - Homo sapiens
Macrophage colony-stimulating factor 1 receptor
Kinase
Kd 6.68 - Homo sapiens
Insulin-like growth factor 1 receptor
Kinase
Kd 6.11 - Homo sapiens
Insulin receptor
Kinase
Kd 6.47 - Homo sapiens
Fibroblast growth factor receptor 3
Kinase
Kd 5.57 - Homo sapiens
Rho-associated protein kinase 1
Kinase
Kd 5.43 - Homo sapiens
Focal adhesion kinase 1
Kinase
Kd 6.51 - Homo sapiens
Tyrosine-protein kinase JAK1
Kinase
Kd 6.48 - Homo sapiens
High affinity nerve growth factor receptor
Kinase
Kd 7.02 - Homo sapiens
Tyrosine-protein kinase JAK2
Kinase
Kd 6.54 - Homo sapiens
Rho-associated protein kinase 2
Kinase
Kd 5.48 - Homo sapiens
Tyrosine-protein kinase SYK
Kinase
Kd 5.6 - Homo sapiens
Angiopoietin-1 receptor
Kinase
Kd 6.57 - Homo sapiens
Ephrin type-A receptor 8
Kinase
Kd 6.55 - Homo sapiens
AP2-associated protein kinase 1
Kinase
Kd 5.64 - Homo sapiens
Hepatocyte growth factor receptor
Kinase
Kd 9.26 - Homo sapiens
Tyrosine-protein kinase Lyn
Kinase
Kd 6.03 - Homo sapiens
Cytoplasmic tyrosine-protein kinase BMX
Kinase
Kd 5.44 - Homo sapiens
LIM domain kinase 1
Kinase
Kd 6.08 - Homo sapiens
5'-AMP-activated protein kinase catalytic subunit alpha-1
Kinase
Kd 5.62 - Homo sapiens
Serine/threonine-protein kinase 10
Kinase
Kd 7.36 - Homo sapiens
Tyrosine-protein kinase Fer
Kinase
Kd 6.57 - Homo sapiens
Serine/threonine-protein kinase PLK4
Kinase
Kd 7.22 - Homo sapiens
Aurora kinase C
Kinase
Kd 5.37 - Homo sapiens
Abelson tyrosine-protein kinase 2
Kinase
Kd 6.34 - Homo sapiens
Ephrin type-A receptor 5
Kinase
Kd 6 - Homo sapiens
Ephrin type-A receptor 4
Kinase
Kd 6.44 - Homo sapiens
Ephrin type-A receptor 6
Kinase
Kd 7.19 - Homo sapiens
Tyrosine-protein kinase Fgr
Kinase
Kd 6.17 - Homo sapiens
Aurora kinase A
Kinase
Kd 6.59 - Homo sapiens
ALK tyrosine kinase receptor
Kinase
Ki 9.13 - Homo sapiens
Ephrin type-A receptor 3
Kinase
Kd 6.15 - Homo sapiens
BMP-2-inducible protein kinase
Kinase
Kd 6.13 - Homo sapiens
Tyrosine-protein kinase FRK
Kinase
Kd 5.54 - Homo sapiens
Mitogen-activated protein kinase kinase kinase kinase 5
Kinase
Kd 7.1 - Homo sapiens
Receptor-interacting serine/threonine-protein kinase 2
Kinase
Kd 6.05 - Homo sapiens
Ephrin type-B receptor 1
Kinase
Kd 6.92 - Homo sapiens
SOURCE DrugCentral 80 associations

Adverse Event Associations

DrugCentral / FAERS disproportionality signal rows matched to this compound.

Reaction PTDrug AE LLRMedDRA
Neoplasm progression 637 1922.725 10061309
Disease progression 897 1779.242 10061818
Death 1078 1167.979 10011906
Visual impairment 261 389.572 10047571
Nausea 710 311.828 10028813
Photopsia 92 301.821 10034962
Oedema peripheral 275 205.486 10030124
Vomiting 458 184.32 10047700
Pleural effusion 191 174.929 10035598
Dysgeusia 126 163.352 10013911
Diarrhoea 516 147.353 10012735
Renal abscess 36 144.909 10038351
Oesophagitis 81 140.323 10030216
Constipation 251 135.295 10010774
Interstitial lung disease 146 134.447 10022611
Pneumonitis 111 133.716 10035742
Drug resistance 95 120.269 10059866
Oedema 144 117.827 10030095
Vitreous floaters 50 114.838 10047654
Metastases to central nervous system 64 112.519 10059282
Acquired gene mutation 32 101.504 10069754
Dysphagia 129 90.248 10013950
Transaminases increased 77 78.813 10054889
Decreased appetite 218 75.933 10061428
Pulmonary embolism 140 74.185 10037377
Renal impairment 131 72.455 10062237
Second primary malignancy 44 68.688 10039801
Malignant neoplasm progression 121 68.188 10051398
Drug ineffective 130 66.235 10013709
Pericardial effusion 66 64.896 10034474
Embolism 40 60.175 10061169
Vision blurred 102 59.063 10047513
Hypoalbuminaemia 44 57.505 10020942
Hepatic function abnormal 75 56.689 10019670
Renal cyst 39 54.757 10038423
Electrocardiogram QT prolonged 83 54.417 10014387
Oesophageal ulcer 28 53.586 10030201
Drug hypersensitivity 9 51.765 10013700
Alanine aminotransferase increased 113 51.048 10001551
Hepatotoxicity 63 50.372 10019851
Renal cyst infection 11 48.272 10058596
Bradycardia 97 48.181 10006093
Arthralgia 51 45.435 10003239
Carcinoembryonic antigen increased 17 43.112 10007266
Aspartate aminotransferase increased 95 42.316 10003481
Rheumatoid arthritis 6 41.491 10039073
Pain 83 38.732 10033371
Sinus bradycardia 36 37.701 10040741
Oesophageal pain 19 37.632 10030180
Therapeutic product effect decreased 3 36.665 10082201

Association rows are source-linked signal records, not incidence rates or clinical causality claims.

SOURCE IUPHAR/BPS 3 interactions

IUPHAR Ligand-Target Data

Curated ligand-target interaction rows with action, affinity, and literature identifiers.

TargetAction AffinityPubMed
ALK receptor tyrosine kinase
ALK
Inhibition 9.0 pIC50 21812414
MET proto-oncogene, receptor tyrosine kinase
MET
Inhibition 8.699999809265137 pKi 21812414
MET proto-oncogene, receptor tyrosine kinase
MET
Inhibition 9.100000381469727 pIC50 21708465
SOURCE PharmGKB 3 phenotype rows

Pharmacogenomics

Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.

ABCB1 (PA267) rs1045642
Genotype AA is associated with increased exposure to crizotinib in people with.
Evidence: -; PMID 27270784
ABCB1 (PA267) rs1128503
Genotype AA is associated with increased exposure to crizotinib in people with.
Evidence: -; PMID 27270784
ABCB1 (PA267) rs2032582
Genotype AA is associated with increased exposure to crizotinib in people with.
Evidence: -; PMID 27270784
SOURCE NLM RxNorm 3 name rows

Drug Names / RxNorm

Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.

NameRxCUI TypeSource
CRIZOTINIB 1148495 SU MTHSPL
crizotinib 1148495 IN RXNORM
Xalkori 1148499 BN RXNORM
SOURCE SIDER 80 side-effect rows

Side Effects

SIDER side-effect terms mapped to the drug or same-CAS compound identity.

Side EffectDrug Name MedDRA TypeConcept ID
Abscess crizotinib LLT C0000833
Abscess crizotinib PT C0000833
Acute respiratory distress syndrome crizotinib LLT C0035222
Acute respiratory distress syndrome crizotinib PT C0035222
Alanine aminotransferase increased crizotinib LLT C0151905
Alanine aminotransferase increased crizotinib PT C0151905
Anaemia crizotinib LLT C0002871
Anaemia crizotinib PT C0002871
Arrhythmia crizotinib LLT C0003811
Arrhythmia crizotinib PT C0003811
Aspartate aminotransferase increased crizotinib LLT C0151904
Aspartate aminotransferase increased crizotinib PT C0151904
Asthenia crizotinib PT C0004093
Balance disorder crizotinib LLT C0575090
Balance disorder crizotinib PT C0575090
Blood alkaline phosphatase increased crizotinib PT C0852911
Blood alkaline phosphatase increased crizotinib LLT C0852911
Blood alkaline phosphatase increased crizotinib PT C0852911
Blood and lymphatic system disorders crizotinib - C0851353
Body temperature increased crizotinib LLT C0015967
Body temperature increased crizotinib PT C0015967
Bradycardia crizotinib LLT C0428977
Bradycardia crizotinib PT C0428977
Burning sensation crizotinib LLT C0085624
Burning sensation crizotinib PT C0085624
Cardiac disorder crizotinib LLT C0018799
Cardiac disorder crizotinib PT C0018799
Congenital renal cyst crizotinib LLT C0268800
Congenital renal cyst crizotinib PT C0268800
Constipation crizotinib LLT C0009806
Constipation crizotinib PT C0009806
Decreased appetite crizotinib LLT C0232462
Decreased appetite crizotinib PT C0232462
Dermatitis crizotinib PT C0011603
Diarrhoea crizotinib LLT C0011991
Diarrhoea crizotinib PT C0011991
Diplopia crizotinib LLT C0012569
Diplopia crizotinib PT C0012569
Disease progression crizotinib LLT C0242656
Disease progression crizotinib PT C0242656
Disorder sight crizotinib LLT C0042790
Dizziness crizotinib LLT C0012833
Dizziness crizotinib PT C0012833
Dizziness crizotinib PT C0012833
Dizziness postural crizotinib LLT C0234987
Dizziness postural crizotinib PT C0234987
Drug-induced liver injury crizotinib LLT C0860207
Drug-induced liver injury crizotinib PT C0860207
Dysaesthesia crizotinib LLT C0392699
Dysaesthesia crizotinib PT C0392699
Dysgeusia crizotinib LLT C0013378
Dysgeusia crizotinib PT C0013378
Dyspepsia crizotinib LLT C0013395
Dyspepsia crizotinib PT C0013395
Dyspnoea crizotinib LLT C0013404
Dyspnoea crizotinib PT C0013404
Electrocardiogram QT corrected interval prolonged crizotinib LLT C0855333
Electrocardiogram QT prolonged crizotinib LLT C0151878
Electrocardiogram QT prolonged crizotinib PT C0151878
Electrocardiogram QT prolonged crizotinib PT C0151878
Eye disorder crizotinib LLT C0015397
Eye disorder crizotinib PT C0015397
Face oedema crizotinib LLT C0542571
Face oedema crizotinib PT C0542571
Fatal outcomes crizotinib - C0206277
Fatigue crizotinib LLT C0015672
Fatigue crizotinib PT C0015672
Febrile neutropenia crizotinib LLT C0746883
Febrile neutropenia crizotinib PT C0746883
Fluid retention crizotinib PT C0268000
Gait disturbance crizotinib LLT C0575081
Gait disturbance crizotinib PT C0575081
Gamma-glutamyltransferase increased crizotinib LLT C0151662
Gamma-glutamyltransferase increased crizotinib PT C0151662
Gastrointestinal disorder crizotinib LLT C0017178
Gastrointestinal disorder crizotinib PT C0017178
Gastrointestinal perforation crizotinib LLT C0151664
Gastrointestinal perforation crizotinib PT C0151664
Generalised oedema crizotinib LLT C0151603
Generalised oedema crizotinib PT C0151603
SOURCE Rendered pharma page rows FAQPage JSON-LD

Frequently Asked Questions

Short answers generated only from the same visible source-linked rows on this page.

What is Crizotinib used for in pharmaceutical contexts?

Crizotinib (CAS 877399-52-5) is rendered as a pharmaceutical compound from the matched source rows; no DailyMed product-name rows are present in this page query.

What are the known adverse events for Crizotinib?

Crizotinib has 674 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Neoplasm progression, Disease progression, Death, Visual impairment, Nausea. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.

Is Crizotinib also used in cosmetics?

No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Crizotinib.

What clinical phase is Crizotinib in?

No phase 1-4 clinical development badge is rendered for Crizotinib because the matched compound identifier rows do not contain a max-phase value.

What bioactivity targets are documented for Crizotinib?

Crizotinib has 158 bioactivity rows in this page query. Rendered target entries include Tyrosine-protein kinase JAK3, Macrophage-stimulating protein receptor, Tyrosine-protein kinase ABL1, Mast/stem cell growth factor receptor Kit, Epidermal growth factor receptor.