Abstract

Crizotinib is a potent small-molecule inhibitor of ALK tyrosine kinase receptor (anaplastic lymphoma kinase; ALK) and hepatocyte growth factor receptor (HGF receptor, proto-oncogene c-Met). A range of tumors, including subsets of non-small cell lung cancer (NSCLC), anaplastic large cell lymphoma and inflammatory myofibroblastic tumors harbor an ALK rearrangement that leads to oncogenic activation of ALK. Crizotinib has demonstrated preclinical and clinical activity against such malignancies through inhibition of ALK, and patients harboring ALK- rearranged NSCLC have demonstrated high response rates and prolonged progression-free survival in phase I and II studies. In August 2011, crizotinib was approved for the treatment of advanced ALK-positive NSCLC.

Links

Publisher Full Text

Authors

Bowles DW, Weickhardt AJ, Doebele RC, Camidge DR, Jimeno A

Institution

University of Colorado School of Medicine, Division of Medical Oncology, Aurora, Colorado 80045, USA.

Source

Drugs of today (Barcelona, Spain : 1998) 48:4 2012 Apr pg 271-82

MeSH

Animals
Antineoplastic Agents
Carcinoma, Non-Small-Cell Lung
Drug Interactions
Drug Resistance, Neoplasm
Evidence-Based Medicine
Humans
Lung Neoplasms
Molecular Targeted Therapy
Protein Kinase Inhibitors
Proto-Oncogene Proteins c-met
Pyrazoles
Pyridines
Receptor Protein-Tyrosine Kinases
Treatment Outcome

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

22536569