Abstract
In August 2011 crizotinib (Xalkori; Pfizer), a small-molecule kinase inhibitor, was approved by the US Food and Drug Administration (FDA) for the treatment of patients with locally advanced or metastatic non-small-cell lung cancer that is anaplastic lymphoma kinase-positive, as detected by an FDA-approved test.
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References
Janku, F. et al. Targeted therapy in non-small-cell lung cancer — is it becoming a reality? Nature Rev. Clin. Oncol. 7, 401–414 (2010).
Soda, M. et al. Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer. Nature 448, 561–567 (2007).
McDermott, U. et al. Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res. 68, 3389–3395 (2008).
Zou, H. Y. et al. An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms. Cancer Res. 67, 4408–4417 (2007).
Cui, J. J. et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition Factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J. Med. Chem. 54, 6342–6363 (2011).
US Food and Drug Administration. FDA labeling information — Xalkori. FDA website [online], (2011).
Kwak, E. L. et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N. Engl. J. Med. 363, 1693–1703 (2010).
Camidge, D. R. et al. Progression-free survival (PFS) from a phase 1 study of crizotinib (PF-02341066) in patients with ALK-positive non-small cell lung cancer (NSCLC). J. Clin. Oncol. 29, 2501 (2011).
Shaw, A. T. et al. Effect of crizotinib on overall survival in patients with advanced non-small-cell lung cancer harbouring ALK gene rearrangement: a retrospective analysis. Lancet Oncol. 12, 1004–1012 (2011).
Choi, Y, L. et al. EML4–ALK mutations in lung cancer that confer resistance to ALK inhibitors. N. Engl. J. Med. 363, 1734–1739 (2010).
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Alice T. Shaw has been a consultant for Pfizer, Chugai and Ariad.
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Shaw, A., Yasothan, U. & Kirkpatrick, P. Crizotinib. Nat Rev Drug Discov 10, 897–898 (2011). https://doi.org/10.1038/nrd3600
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DOI: https://doi.org/10.1038/nrd3600
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