PMID- 27912760
OWN - NLM
STAT- MEDLINE
DCOM- 20170303
LR  - 20220310
IS  - 1423-0127 (Electronic)
IS  - 1021-7770 (Print)
IS  - 1021-7770 (Linking)
VI  - 23
IP  - 1
DP  - 2016 Dec 3
TI  - Update on recent preclinical and clinical studies of T790M mutant-specific 
      irreversible epidermal growth factor receptor tyrosine kinase inhibitors.
PG  - 86
LID - 86
AB  - The first- and second-generation epidermal growth factor receptor tyrosine kinase 
      inhibitors (1/2G EGFR-TKIs) gefitinib, erlotinib, and afatinib have all been 
      approved as standard first-line treatments for advanced EGFR mutation-positive 
      non-small cell lung cancer. The third-generation (3G) EGFR-TKIs have been 
      developed to overcome the EGFR T790M mutation, which is the most common mechanism 
      of acquired resistance to 1/2G EGFR-TKI treatment. This resistance mutation 
      develops in half of the patients who respond to 1/2G EGFR-TKI therapy. The 
      structures of the novel 3G EGFR-TKIs are different from those of 1/2G EGFR-TKIs. 
      Particularly, 3G EGFR-TKIs have lower affinity to wild-type EGFR, and are 
      therefore associated with lower rates of skin and gastrointestinal toxicities. 
      However, many of the adverse events (AEs) that are observed in patients receiving 
      3G EGFR-TKIs have not been observed in patients receiving 1/2G EGFR-TKIs. 
      Although preclinical studies have revealed many possible mechanisms for these 
      AEs, the causes of some AEs remain unknown. Many mechanisms of resistance to 3G 
      EGFR-TKI therapy have also been reported. Here, we have reviewed the recent 
      clinical and preclinical developments related to novel 3G EGFR-TKIs, including 
      osimertinib, rociletinib, olmutinib, EGF816, and ASP8273.
FAU - Liao, Bin-Chi
AU  - Liao BC
AD  - Department of Oncology, National Taiwan University Hospital, 7, Chung-Shan South 
      Road, Taipei, 100, Taiwan.
AD  - National Taiwan University Cancer Center, College of Medicine, National Taiwan 
      University, Taipei, Taiwan.
AD  - Graduate Institute of Clinical Medicine, College of Medicine, National Taiwan 
      University, Taipei, Taiwan.
FAU - Lin, Chia-Chi
AU  - Lin CC
AD  - Department of Oncology, National Taiwan University Hospital, 7, Chung-Shan South 
      Road, Taipei, 100, Taiwan.
AD  - Department of Urology, College of Medicine, National Taiwan University, Taipei, 
      Taiwan.
FAU - Lee, Jih-Hsiang
AU  - Lee JH
AD  - Department of Oncology, National Taiwan University Hospital, 7, Chung-Shan South 
      Road, Taipei, 100, Taiwan.
AD  - Department of Medical Research, National Taiwan University Hospital, Taipei, 
      Taiwan.
FAU - Yang, James Chih-Hsin
AU  - Yang JC
AD  - Department of Oncology, National Taiwan University Hospital, 7, Chung-Shan South 
      Road, Taipei, 100, Taiwan. chihyang@ntu.edu.tw.
AD  - National Taiwan University Cancer Center, College of Medicine, National Taiwan 
      University, Taipei, Taiwan. chihyang@ntu.edu.tw.
AD  - Graduate Institute of Clinical Medicine, College of Medicine, National Taiwan 
      University, Taipei, Taiwan. chihyang@ntu.edu.tw.
AD  - Graduate Institute of Oncology, College of Medicine, National Taiwan University, 
      Taipei, Taiwan. chihyang@ntu.edu.tw.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20161203
PL  - England
TA  - J Biomed Sci
JT  - Journal of biomedical science
JID - 9421567
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Protein Kinase Inhibitors)
RN  - EC 2.7.10.1 (ErbB Receptors)
SB  - IM
MH  - Antineoplastic Agents/*pharmacology/*therapeutic use
MH  - Carcinoma, Non-Small-Cell Lung/*drug therapy/enzymology
MH  - Clinical Trials as Topic
MH  - Drug Resistance, Neoplasm/*drug effects/genetics
MH  - ErbB Receptors/*antagonists & inhibitors/genetics
MH  - Humans
MH  - *Mutation
MH  - Protein Kinase Inhibitors/*pharmacology/*therapeutic use
PMC - PMC5135794
OTO - NOTNLM
OT  - ASP8273
OT  - EGF816
OT  - Epidermal growth factor receptor
OT  - Non-small cell lung cancer
OT  - Olmutinib
OT  - Osimertinib
OT  - Rociletinib
OT  - T790M mutation
OT  - Tyrosine kinase inhibitor
EDAT- 2016/12/04 06:00
MHDA- 2017/03/04 06:00
PMCR- 2016/12/03
CRDT- 2016/12/04 06:00
PHST- 2016/08/19 00:00 [received]
PHST- 2016/11/03 00:00 [accepted]
PHST- 2016/12/04 06:00 [entrez]
PHST- 2016/12/04 06:00 [pubmed]
PHST- 2017/03/04 06:00 [medline]
PHST- 2016/12/03 00:00 [pmc-release]
AID - 10.1186/s12929-016-0305-9 [pii]
AID - 305 [pii]
AID - 10.1186/s12929-016-0305-9 [doi]
PST - epublish
SO  - J Biomed Sci. 2016 Dec 3;23(1):86. doi: 10.1186/s12929-016-0305-9.