Next-generation epidermal growth factor receptor tyrosine kinase inhibitors in epidermal growth factor receptor -mutant non-small cell lung cancer

Highlights • 3rd generation EGFR TKIs are T790M selective with minimal inhibition in WT EGFR. • The 3rd generation EGFR TKIs are highly active and are well tolerated. • Acquired resistance to 3rd generation EGFR TKIs include EGFR C797S mutation. • A new class of EGFR TKI has increased CNS penetratio...

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Veröffentlicht in:	Lung cancer (Amsterdam, Netherlands) Netherlands), 2016-03, Vol.93, p.59-68
Hauptverfasser:	Tan, Chee-Seng, Cho, Byoung-Chul, Soo, Ross A
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Antineoplastic Combined Chemotherapy Protocols - therapeutic use Blood-Brain Barrier - drug effects Blood-Brain Barrier - metabolism Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - genetics Carcinoma, Non-Small-Cell Lung - mortality Carcinoma, Non-Small-Cell Lung - pathology Clinical Trials as Topic Drug Discovery Drug Evaluation, Preclinical Epidermal growth factor receptor mutations Hematology, Oncology and Palliative Medicine HM61713 Humans Lung Neoplasms - drug therapy Lung Neoplasms - genetics Lung Neoplasms - mortality Lung Neoplasms - pathology Molecular Targeted Therapy Mutation Non-small cell lung cancer Osimertinib Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Pulmonary/Respiratory Receptor, Epidermal Growth Factor - antagonists & inhibitors Receptor, Epidermal Growth Factor - genetics Rociletinib Treatment Outcome Tyrosine kinase inhibitor
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Zusammenfassung:	Highlights • 3rd generation EGFR TKIs are T790M selective with minimal inhibition in WT EGFR. • The 3rd generation EGFR TKIs are highly active and are well tolerated. • Acquired resistance to 3rd generation EGFR TKIs include EGFR C797S mutation. • A new class of EGFR TKI has increased CNS penetration with promising CNS activity.
ISSN:	0169-5002 1872-8332
DOI:	10.1016/j.lungcan.2016.01.003