HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Crizotinib.

Abstract
Crizotinib is an ATP-competitive small-molecule inhibitor of the receptor tyrosine kinases (RTK) c-Met, anaplastic lymphoma kinase (ALK), and ROS1. There is convincing clinical evidence for the effectiveness in non-small-cell lung cancer (NSCLC) harboring EML4-ALK rearrangements resulting in constitutional activation of the ALK-RTK. The drug is approved for this entity, which represents no more than 3-5% of all NSCLC. However, in this population, impressive response rates are generated. The same seems to be true for ROS-1 rearrangements; however, these only occur in approximately 1% of all NSCLC. The role in c-Met altered cancers needs to be determined. Toxicities include visual impairment, nausea, peripheral edema, QT-prolongation, and liver enzyme elevation. Also, the occurrence of renal cysts is reported. Fluorescence in situ hybridization (FISH) detecting the ALK rearrangement has to be performed on tumor tissue to predict crizotinib efficacy. The role of immunohistochemistry in this setting needs to be determined. It has high concordance with FISH results when strongly positive or completely negative. The high efficacy of crizotinib in ALK- and ROS-positive lung cancer as new molecular targets beside the epidermal growth factor receptor (EGFR) underscores the importance of molecular typing in NSCLC.
AuthorsDavid F Heigener, Martin Reck
JournalRecent results in cancer research. Fortschritte der Krebsforschung. Progres dans les recherches sur le cancer (Recent Results Cancer Res) Vol. 201 Pg. 197-205 ( 2014) ISSN: 0080-0015 [Print] Germany
PMID24756793 (Publication Type: Journal Article, Review)
Chemical References
  • Antineoplastic Agents
  • EML4-ALK fusion protein, human
  • Oncogene Proteins, Fusion
  • Protein Kinase Inhibitors
  • Pyrazoles
  • Pyridines
  • Crizotinib
Topics
  • Animals
  • Antineoplastic Agents (therapeutic use)
  • Carcinoma, Non-Small-Cell Lung (drug therapy, genetics)
  • Crizotinib
  • Humans
  • Lung Neoplasms (drug therapy, genetics)
  • Oncogene Proteins, Fusion (drug effects)
  • Protein Kinase Inhibitors (therapeutic use)
  • Pyrazoles (therapeutic use)
  • Pyridines (therapeutic use)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: