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
- Research Support, Non-U.S. Gov't
- Review
MeSH terms
- Aminopyridines
- Anaplastic Lymphoma Kinase
- Carbazoles / therapeutic use
- Carcinoma, Non-Small-Cell Lung / drug therapy*
- Carcinoma, Non-Small-Cell Lung / enzymology
- Carcinoma, Non-Small-Cell Lung / pathology
- Humans
- Kaplan-Meier Estimate
- Lactams
- Lactams, Macrocyclic / therapeutic use
- Lung Neoplasms / drug therapy*
- Lung Neoplasms / enzymology
- Lung Neoplasms / pathology
- Organophosphorus Compounds / therapeutic use
- Piperidines / therapeutic use
- Protein Kinase Inhibitors / therapeutic use*
- Pyrazoles
- Pyrimidines / therapeutic use
- Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
- Receptor Protein-Tyrosine Kinases / genetics
- Receptor Protein-Tyrosine Kinases / metabolism
- Sulfones / therapeutic use
Substances
- Aminopyridines
- Carbazoles
- Lactams
- Lactams, Macrocyclic
- Organophosphorus Compounds
- Piperidines
- Protein Kinase Inhibitors
- Pyrazoles
- Pyrimidines
- Sulfones
- ALK protein, human
- Anaplastic Lymphoma Kinase
- Receptor Protein-Tyrosine Kinases
- brigatinib
- ceritinib
- alectinib
- lorlatinib