Next Article in Journal
Ethanol Impairs NRF2/Antioxidant and Growth Signaling in the Intact Placenta In Vivo and in Human Trophoblasts
Previous Article in Journal
Unravelling the Skin Secretion Peptides of the Gliding Leaf Frog, Agalychnis spurrelli (Hylidae)
Open AccessReview

FDA- and EMA-Approved Tyrosine Kinase Inhibitors in Advanced EGFR-Mutated Non-Small Cell Lung Cancer: Safety, Tolerability, Plasma Concentration Monitoring, and Management

1
Unité de Recherche Translationnelle, Institut du Cancer de Montpellier (ICM), 34000 Montpellier, France
2
Département de Pharmacie, Institut du Cancer de Montpellier (ICM), 34000 Montpellier, France
3
Service d’Oncologie Médicale, Institut du Cancer de Montpellier (ICM), IRCM, INSERM, Univ. Montpellier, 34000 Montpellier, France
*
Author to whom correspondence should be addressed.
Biomolecules 2019, 9(11), 668; https://doi.org/10.3390/biom9110668
Received: 8 October 2019 / Revised: 23 October 2019 / Accepted: 25 October 2019 / Published: 30 October 2019
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. View Full-Text
Keywords: TKIs; NSCLC; side effects; TDM; quantification TKIs; NSCLC; side effects; TDM; quantification
MDPI and ACS Style

Solassol, I.; Pinguet, F.; Quantin, X. FDA- and EMA-Approved Tyrosine Kinase Inhibitors in Advanced EGFR-Mutated Non-Small Cell Lung Cancer: Safety, Tolerability, Plasma Concentration Monitoring, and Management. Biomolecules 2019, 9, 668.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop