Abstract
Crizotinib as the first-generation ALK inhibitor has shown significant activity in ALK-mutated non-small cell lung cancer (NSCLC). Second- and third-generation ALK inhibitors are entering clinical applications for ALK+ NSCLC. In addition, a third-generation ALK inhibitor, lorlatinib (PF-06463922), was reported to resensitize NSCLC to crizotinib. This review provided a summary of clinical development of alectinib, ceritinib, brigatinib (AP26113), and lorlatinib.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Aminopyridines
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Anaplastic Lymphoma Kinase
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Carbazoles / therapeutic use
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Carcinoma, Non-Small-Cell Lung / drug therapy*
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Carcinoma, Non-Small-Cell Lung / enzymology
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Carcinoma, Non-Small-Cell Lung / pathology
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Humans
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Kaplan-Meier Estimate
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Lactams
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Lactams, Macrocyclic / therapeutic use
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Lung Neoplasms / drug therapy*
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Lung Neoplasms / enzymology
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Lung Neoplasms / pathology
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Organophosphorus Compounds / therapeutic use
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Piperidines / therapeutic use
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Protein Kinase Inhibitors / therapeutic use*
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Pyrazoles
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Pyrimidines / therapeutic use
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Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
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Receptor Protein-Tyrosine Kinases / genetics
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Receptor Protein-Tyrosine Kinases / metabolism
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Sulfones / therapeutic use
Substances
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Aminopyridines
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Carbazoles
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Lactams
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Lactams, Macrocyclic
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Organophosphorus Compounds
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Piperidines
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Protein Kinase Inhibitors
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Pyrazoles
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Pyrimidines
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Sulfones
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ALK protein, human
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Anaplastic Lymphoma Kinase
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Receptor Protein-Tyrosine Kinases
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brigatinib
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ceritinib
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alectinib
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lorlatinib