Comparison of the Efficacy of EGFR Tyrosine Kinase Inhibitors Erlotinib and Low-dose Osimertinib on a PC-9-GFP
Acrylamides
/ administration & dosage
Aniline Compounds
/ administration & dosage
Animals
Brain Neoplasms
/ drug therapy
Carcinoma, Non-Small-Cell Lung
/ genetics
Cell Line, Tumor
Disease Models, Animal
Drug Synergism
Drug Therapy, Combination
ErbB Receptors
/ genetics
Erlotinib Hydrochloride
/ administration & dosage
Female
Genes, Reporter
Lung Neoplasms
/ genetics
Male
Mice
Mice, Nude
Mutation
Protein Kinase Inhibitors
/ administration & dosage
Treatment Outcome
Xenograft Model Antitumor Assays
Erlotinib
PC-9-GFP
non-small cell lung cancer
nude mice
osimertinib
Journal
In vivo (Athens, Greece)
ISSN: 1791-7549
Titre abrégé: In Vivo
Pays: Greece
ID NLM: 8806809
Informations de publication
Date de publication:
Historique:
received:
26
02
2020
revised:
10
03
2020
accepted:
11
03
2020
entrez:
2
5
2020
pubmed:
2
5
2020
medline:
13
2
2021
Statut:
ppublish
Résumé
Brain metastases are found in approximately 30% of patients with epidermal-growth-factor receptor (EGFR) mutant non-small cell lung cancer (NSCLC). We compared the efficacy of two EGFR-tyrosine kinase inhibitors (TKIs), erlotinib and osimertinib on a PC-9-GFP EGFR mutant NSCLC growing in the brain of nude mice. The brain metastasis models were randomized into five groups and treated for 15 days: Control; 5 mg/kg erlotinib; 50 mg/kg erlotinib; 0.5 mg/kg osimertinib; 5 mg/kg osimertinib. Tumor volume was evaluated by non-invasive fluorescence imaging. Only 5 mg/kg osimertinib, a low-dose compared to the clinically-equivalent dose, showed significant tumor regression compared to the control. This study strongly supports the high activity of osimertinib for intracranial lesions of EGFR-mutant NSCLC.
Sections du résumé
BACKGROUND/AIM
OBJECTIVE
Brain metastases are found in approximately 30% of patients with epidermal-growth-factor receptor (EGFR) mutant non-small cell lung cancer (NSCLC). We compared the efficacy of two EGFR-tyrosine kinase inhibitors (TKIs), erlotinib and osimertinib on a PC-9-GFP EGFR mutant NSCLC growing in the brain of nude mice.
MATERIALS AND METHODS
METHODS
The brain metastasis models were randomized into five groups and treated for 15 days: Control; 5 mg/kg erlotinib; 50 mg/kg erlotinib; 0.5 mg/kg osimertinib; 5 mg/kg osimertinib. Tumor volume was evaluated by non-invasive fluorescence imaging.
RESULTS
RESULTS
Only 5 mg/kg osimertinib, a low-dose compared to the clinically-equivalent dose, showed significant tumor regression compared to the control.
CONCLUSION
CONCLUSIONS
This study strongly supports the high activity of osimertinib for intracranial lesions of EGFR-mutant NSCLC.
Identifiants
pubmed: 32354888
pii: 34/3/1027
doi: 10.21873/invivo.11871
pmc: PMC7279826
doi:
Substances chimiques
Acrylamides
0
Aniline Compounds
0
Protein Kinase Inhibitors
0
osimertinib
3C06JJ0Z2O
Erlotinib Hydrochloride
DA87705X9K
EGFR protein, human
EC 2.7.10.1
ErbB Receptors
EC 2.7.10.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
1027-1030Informations de copyright
Copyright© 2020, International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.
Références
Clin Cancer Res. 2016 Oct 15;22(20):5130-5140
pubmed: 27435396
J Clin Oncol. 2018 Aug 28;:JCO2018783118
pubmed: 30153097
N Engl J Med. 2018 Jan 11;378(2):113-125
pubmed: 29151359
Lung Cancer. 2013 Nov;82(2):282-7
pubmed: 24021541
Transl Oncol. 2019 Apr;12(4):640-645
pubmed: 30807997
J Cell Biochem. 1994 Sep;56(1):1-3
pubmed: 7806583
Anticancer Res. 2015 Nov;35(11):5797-806
pubmed: 26504000
Int J Clin Oncol. 2015 Aug;20(4):674-9
pubmed: 25336382
J Clin Oncol. 2018 Sep 10;36(26):2702-2709
pubmed: 30059262