PMID- 31671561
OWN - NLM
STAT- MEDLINE
DCOM- 20200902
LR  - 20200902
IS  - 2218-273X (Electronic)
IS  - 2218-273X (Linking)
VI  - 9
IP  - 11
DP  - 2019 Oct 30
TI  - FDA- and EMA-Approved Tyrosine Kinase Inhibitors in Advanced EGFR-Mutated 
      Non-Small Cell Lung Cancer: Safety, Tolerability, Plasma Concentration 
      Monitoring, and Management.
LID - 10.3390/biom9110668 [doi]
LID - 668
AB  - Non-small-cell lung cancer (NSCLC) is the most common form of primary lung 
      cancer. The discovery of several oncogenic driver mutations in patients with 
      NSCLC has allowed the development of personalized treatments based on these 
      specific molecular alterations, in particular in the tyrosine kinase (TK) domain 
      of the epidermal growth factor receptor (EGFR) gene. Gefitinib, erlotinib, 
      afatinib, and osimertinib are TK inhibitors (TKIs) that specifically target EGFR 
      and are currently approved by the Food and Drug Administration (FDA) and the 
      European Medicines Agency (EMA) as first line treatment for sensitive EGFR-mutant 
      patients. However, these four drugs are associated with severe adverse events 
      (AEs) that can significantly impact patient health-related quality of life and 
      patient monitoring. EGFR-TKIs are commonly used together with other types of 
      medication that can substantially interact. Here, we review approaches used for 
      the management of TKI-AEs in patients with advanced NSCLC to promote the benefits 
      of treatments and minimize the risk of TKI treatment discontinuation. We also 
      consider potential TKI-drug interactions and discuss the usefulness of plasma 
      concentration monitoring TKIs based on chromatographic and mass spectrometry 
      approaches to guide clinical decision-making. Adjusting the most appropriate 
      therapeutic strategies and drug doses may improve the performance therapy and 
      prognosis of patients with advanced EGFR-mutated NSCLC.
FAU - Solassol, Isabelle
AU  - Solassol I
AD  - Unite de Recherche Translationnelle, Institut du Cancer de Montpellier (ICM), 
      34000 Montpellier, France. Isabelle.solassol@icm.unicancer.fr.
AD  - Departement de Pharmacie, Institut du Cancer de Montpellier (ICM), 34000 
      Montpellier, France. Isabelle.solassol@icm.unicancer.fr.
FAU - Pinguet, Frederic
AU  - Pinguet F
AD  - Departement de Pharmacie, Institut du Cancer de Montpellier (ICM), 34000 
      Montpellier, France. frederic.pinguet@icm.unicancer.fr.
FAU - Quantin, Xavier
AU  - Quantin X
AD  - Service d'Oncologie Medicale, Institut du Cancer de Montpellier (ICM), IRCM, 
      INSERM, Univ. Montpellier, 34000 Montpellier, France. 
      xavier.quantin@icm.unicancer.fr.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20191030
PL  - Switzerland
TA  - Biomolecules
JT  - Biomolecules
JID - 101596414
RN  - 0 (Protein Kinase Inhibitors)
RN  - EC 2.7.10.1 (ErbB Receptors)
SB  - IM
MH  - Carcinoma, Non-Small-Cell Lung/blood/*drug therapy/genetics/pathology
MH  - Drug Approval
MH  - ErbB Receptors/*antagonists & inhibitors
MH  - Europe
MH  - Humans
MH  - Lung Neoplasms/blood/*drug therapy/genetics/pathology
MH  - *Mutation
MH  - Protein Kinase Inhibitors/adverse effects/blood/*pharmacology/therapeutic use
MH  - *Safety
MH  - United States
MH  - United States Food and Drug Administration/*legislation & jurisprudence
PMC - PMC6921037
OTO - NOTNLM
OT  - NSCLC
OT  - TDM
OT  - TKIs
OT  - quantification
OT  - side effects
COIS- The authors declare no conflict of interest.
EDAT- 2019/11/02 06:00
MHDA- 2020/09/04 06:00
PMCR- 2019/11/01
CRDT- 2019/11/02 06:00
PHST- 2019/10/08 00:00 [received]
PHST- 2019/10/23 00:00 [revised]
PHST- 2019/10/25 00:00 [accepted]
PHST- 2019/11/02 06:00 [entrez]
PHST- 2019/11/02 06:00 [pubmed]
PHST- 2020/09/04 06:00 [medline]
PHST- 2019/11/01 00:00 [pmc-release]
AID - biom9110668 [pii]
AID - biomolecules-09-00668 [pii]
AID - 10.3390/biom9110668 [doi]
PST - epublish
SO  - Biomolecules. 2019 Oct 30;9(11):668. doi: 10.3390/biom9110668.