Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 24, Issue 4, Pages 417-442Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543776.2014.877890
Keywords
anaplastic large-cell lymphoma; anaplastic lymphoma kinase; cancer; non-small-cell lung cancer; small-molecule inhibitors
Categories
Ask authors/readers for more resources
Introduction: Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase from the insulin receptor superfamily, is implicated in the oncogenesis of numerous cancers including anaplastic large-cell lymphoma, non-small-cell lung cancer, diffuse large B-cell lymphoma, inflammatory myofibroblastic tumors, glioblastoma, as well as neuroblastoma. The root cause for these specific cancers has been identified as aberrant ALK kinase activity, which has been shown to be associated with specific gene translocations, single-point mutations, gene amplification and/or overexpression. The direct inhibition of ALK with small-molecule inhibitors represents a viable therapeutic intervention that has achieved clinical proof of concept. Areas covered: Small-molecule ALK inhibitors covered in the patent literature from 2010 to September 2013 are described. Relevant peer-reviewed journal articles that describe discovery and development of the above-identified ALK inhibitors are also discussed. Keyword-based (e. g., ALK, anaplastic lymphoma kinase) literature searches were conducted in Scifinder (R). Expert opinion: Novel ALK inhibitors continued to be discovered at a fast pace over the covered period, with many distinct chemotypes emerging. Crizotinib received FDA approval in 2011, and six additional ALK inhibitors have entered clinical trials. The focus of ALK research appears to have shifted toward inhibitors that display activity against resistant mutants unearthed in clinical studies with crizotinib.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available