Cancer II pp 435-467 | Cite as

Small Molecule Inhibitors of ALK

  • John M. Hatcher
  • Nathanael S. GrayEmail author
Part of the Topics in Medicinal Chemistry book series (TMC, volume 28)


Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that has attracted a great deal of attention due to its oncogenic potential and essential role in the pathogenesis of a wide variety of human cancers, such as anaplastic large cell lymphomas (ALCLs), non-small cell lung cancer (NSCLC), breast cancer, colorectal cancer, neuroblastoma, and ovarian cancer. Despite the remarkable clinical success of crizotinib (Xalkori), the first ALK inhibitor approved in 2011 for the treatment of NSCLC, the emergence of resistance mutations frequently causes relapse in patients. As a result, a variety of second and third generation ALK inhibitors have been developed to overcome these mutations. This chapter presents an overview of the hit-to-drug evolution strategies as well as the biological activities of several second and third generation ALK inhibitors.


ALK inhibitor Anaplastic large cell lymphomas (ALCLs) Anaplastic lymphoma kinase (ALK) Non-small cell lung cancer (NSCLC) 



We wish to thank Chelsea Powell for critical reading and editing of this chapter.


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Copyright information

© Springer International Publishing AG 2017

Authors and Affiliations

  1. 1.Longwood CenterDana Farber Cancer InstituteBostonUSA

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