crizotinib
Trade name: xalkori
Small moleculeapprovedOrphan Drug FDA
Approved
Aug 26, 2011
Crizotinib (trade name Xalkori, Pfizer, Inc.) is an anti cancer drug approved for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d’Origine Nantais (RON). Common adverse reactions in clinical trials with crizotinib, occurring at an incidence of 25% or higher, included visual disorders, nausea, diarrhea, vomiting, constipation, edema, elevated transaminases, and fatigue. Crizotinib is currently under investigational study for use in treatment of Uveal Melanoma. — NCATS
Clinical trial activity
131 trials · 125 clinical orgs · 1 marketing orgs
Phase 1
50
Phase 2
69
Phase 3
22
Phase 4
4
Earliest trial started Apr 26, 2006 (NCT00585195)
Timeline
2000s
Indications
Studied for
- Adenocarcinoma · Phase 2
- Adenocarcinoma of Lung · Phase 2
- Asthma · Phase 3
- Bile Duct Neoplasms · Phase 2
- Biomarkers · Phase 3
- Brain Neoplasms · Phase 2
- Breast Neoplasms · Phase 2/Phase 3
- Carcinoma · Phase 3
- Carcinoma, Hepatocellular · Phase 1
- Carcinoma, Large Cell · Phase 1
- Carcinoma, Renal Cell · Phase 2
- Carcinoma, Squamous Cell · Phase 2
- Carotid Intima-Media Thickness · Phase 4
- Colonic Neoplasms · Phase 2
- Colorectal Neoplasms · Phase 2
- Coronary Artery Disease · Phase 1
- Crizotinib · Phase 2
- Diabetes Mellitus, Type 2 · Phase 1
- Diffuse Intrinsic Pontine Glioma · Phase 1
- Drug Therapy · Phase 3
- Endometrial Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 2
- Gallbladder Neoplasms · Phase 2
- Glioblastoma · Phase 1
- Glioma · Phase 2
- Healthy Volunteers · Phase 1
- Heart Failure · Phase 1
- HIV Infections · Phase 1
- Kidney Failure, Chronic · Phase 1
- Kidney Neoplasms · Phase 2
- Leukemia · Phase 1
- Leukemia, Myeloid, Acute · Phase 2
- Liver Neoplasms · Phase 2
- Lung Neoplasms · Phase 3
- Lymphoma · Phase 3
- Lymphoma, Large-Cell, Anaplastic · Phase 4
- Lymphoma, Non-Hodgkin · Phase 2
- Melanoma · Phase 2/Phase 3
- Multiple Myeloma · Phase 2
- Mutation · Phase 2
- Neoplasm Metastasis · Phase 2
- Neuroblastoma · Phase 1/Phase 2
- Neurofibroma · Phase 1
- Neurofibromatosis 2 · Phase 2
- Oncogene Proteins · Phase 2
- Oncogenes · Phase 3
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Pharmacokinetics · Phase 2
- Prostatic Neoplasms · Phase 2
- Prostatic Neoplasms, Castration-Resistant · Phase 1
- Proto-Oncogene Proteins c-met · Phase 2
- Pulmonary Disease, Chronic Obstructive · Phase 1
- Rhabdomyosarcoma · Phase 2
- Skin Neoplasms · Phase 2
- Small Cell Lung Carcinoma · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
- Thyroid Neoplasms · Phase 2
- Triple Negative Breast Neoplasms · Phase 2
- Ureteral Neoplasms · Phase 2
- Urethral Neoplasms · Phase 2
- Urinary Bladder Neoplasms · Phase 2
- Uterine Cervical Neoplasms · Phase 2
- Uterine Neoplasms · Phase 2
- Vestibular Diseases · Phase 2
Mechanism of action
- EML4-ALK INHIBITOR
EML4-ALK
NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor)
Macrophage-stimulating protein receptor inhibitor
Proto-oncogene tyrosine-protein kinase ROS inhibitor
- Hepatocyte growth factor receptorINHIBITOR
MET inhibitor
- ALK tyrosine kinase receptorINHIBITOR
ALK inhibitor
Approval history
- approvedPriority reviewAcceleratedAug 26, 2011
Chemistry & pharmacology
Loading structure…
SMILES
C[C@@H](OC1=CC(=CN=C1N)C2=CN(N=C2)C3CCNCC3)C4=C(Cl)C=CC(F)=C4Cl- Mol. weight
- 450.337 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
First in class
Sources
- WikipediaCrizotinib ↗
- NCATS53AH36668S ↗
- ChEMBLCHEMBL601719 ↗
Also known as
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinib
- crizotinibum
- crizotinibum
- pf02341066
- pf 02341066
- pf 02341066
- pf-02341066
- pf-02341066
- pf-02341066
- pf-02341066
- pf-2341066
- pf-2341066
- pf-2341066
- (r)-crizotinib
- (r)-crizotinib
- xalkori
- xalkori
- xalkori
- xalkori
- xalkori
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06563999 | Phase 2 | Dec 1, 2024 | Sun Yat-Sen University |
| NCT06564324 | Phase 3 | Sep 30, 2024 | AnHeart Therapeutics Inc., Huazhong University of Science and Technology |
| NCT06254599 | Phase 3 | May 1, 2024 | Government of China |
| NCT06062810 | Phase 2/Phase 3 (Phase 3) | Mar 28, 2024 | Medicine Invention Design, Inc |
| NCT06322095 | Phase 2 | Mar 22, 2024 | Suzhou Genhouse Bio Co., Ltd. |
| NCT06140836 | Phase 3 | Jan 15, 2024 | Bristol-Myers Squibb, Zai Lab Pty. Ltd. |
| NCT06082635 | Phase 3 | Nov 30, 2023 | Government of China, Sun Yat-Sen University |
| NCT05987332 | Phase 2/Phase 3 (Phase 3) | Oct 31, 2023 | IDEAYA Biosciences |
| NCT05725200 | Phase 2 | Sep 27, 2022 | University of Oslo |
| NCT05204628 | Phase 3 | Feb 7, 2022 | Jilin University, Xuanzhu Biopharmaceutical Co., Ltd. |
| NCT05160922 | Phase 4 | Dec 31, 2021 | Pfizer |
| NCT06569420 | Phase 3 | Dec 31, 2021 | Fosun |
| NCT05014464 | Phase 2 | Nov 13, 2021 | Central South University |
| NCT05122143 | N/A | Nov 10, 2021 | Altamira Medica Ltd., Cliantha Research Limited |
| NCT04603807 | Phase 3 | Apr 30, 2021 | Roche |
| NCT04856293 | Phase 1 | Apr 16, 2021 | Pfizer |
| NCT04693468 | Phase 1 | Dec 1, 2020 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT04600505 | Phase 1 | Oct 19, 2020 | AstraZeneca, Parexel |
| NCT04489134 | Phase 2 | Sep 30, 2020 | University of Rennes |
| NCT04970940 | Phase 1 | Jul 2, 2020 | Aju Pharm, Jeonbuk National University |
Showing 20 of 131 trials
Page 1 / 7
Organizations
Research & Development (125)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 53 | 35 | 5 | 2006 |
| National Cancer Institute (NCI) | Government | 16 | 13 | 4 | 2009 |
| AstraZeneca | For profit | 7 | 4 | 2 | 2015 |
| ECOG-ACRIN Cancer Research Group | Academic/Hospital | 6 | 1 | 2 | 2014 |
| Roche | For profit | 6 | 4 | 2 | 2014 |
| Bristol-Myers Squibb | For profit | 5 | 2 | 3 | 2013 |
| University of Texas at Houston | Academic/Hospital | 4 | 4 | 1 | 2012 |
| Central South University | Academic/Hospital | 3 | 3 | 1 | 2020 |
| Parexel | For profit | 3 | 0 | 1 | 2018 |
| People's Liberation Army of China | Government | 3 | 2 | 3 | 2015 |
| Sun Yat-Sen University | Academic/Hospital | 3 | 1 | 2 | 2019 |
| Array BioPharma | For profit | 2 | 0 | 2 | 2014 |
| Chiesi | For profit | 2 | 2 | 2 | 2019 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 2 | 1 | 2 | 2015 |
| Eastern Hepatobiliary Surgery Hospital | Academic/Hospital | 2 | 0 | 1 | 2016 |
| Fudan University | Academic/Hospital | 2 | 0 | 1 | 2016 |
| GlaxoSmithKline | For profit | 2 | 0 | 2 | 2018 |
| Government of China | Government | 2 | 2 | 1 | 2023 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2014 |
| Institut Gustave Roussy | Academic/Hospital | 2 | 0 | 1 | 2012 |
125 organizations
Page 1 / 7