Acquired resistance to TKIs in solid tumours: learning from lung cancer

DR Camidge, W Pao, LV Sequist - Nature reviews Clinical oncology, 2014 - nature.com
The use of advanced molecular profiling to direct the use of targeted therapy, such as
tyrosine kinase inhibitors (TKIs) for patients with advanced-stage non-small-cell lung cancer …

Rational, biologically based treatment of EGFR-mutant non-small-cell lung cancer

W Pao, J Chmielecki - Nature Reviews Cancer, 2010 - nature.com
Epidermal growth factor receptor (EGFR)-mutant non-small-cell lung cancer (NSCLC) was
first recognized in 2004 as a distinct, clinically relevant molecular subset of lung cancer. The …

Adjuvant erlotinib versus placebo in patients with stage IB-IIIA non–small-cell lung cancer (RADIANT): A randomized, double-blind, phase III trial

K Kelly, NK Altorki, WEE Eberhardt… - Journal of Clinical …, 2015 - ascopubs.org
Purpose Epidermal growth factor receptor (EGFR)–tyrosine kinase inhibitors have proven
efficacy in advanced non–small-cell lung cancer (NSCLC). We hypothesized that erlotinib …

Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer

H Yasuda, E Park, CH Yun, NJ Sng… - Science translational …, 2013 - science.org
Epidermal growth factor receptor (EGFR) gene mutations (G719X, exon 19
deletions/insertions, L858R, and L861Q) predict favorable responses to EGFR tyrosine …

CSF concentration of the anaplastic lymphoma kinase inhibitor crizotinib

DB Costa, S Kobayashi, SS Pandya, WL Yeo… - Journal of Clinical …, 2011 - ascopubs.org
Discussion Crizotinib (molecular weight, 450.34) is an anaplastic lymphoma kinase (ALK)
tyrosine kinase inhibitor (TKI) 3 that leads to responses in most patients with NSCLC …

Optimization of dosing for EGFR-mutant non–small cell lung cancer with evolutionary cancer modeling

J Chmielecki, J Foo, GR Oxnard… - Science translational …, 2011 - science.org
Non–small cell lung cancers (NSCLCs) that harbor mutations within the epidermal growth
factor receptor (EGFR) gene are sensitive to the tyrosine kinase inhibitors (TKIs) gefitinib …

Comparison of gefitinib, erlotinib and afatinib in non‐small cell lung cancer: a meta‐analysis

Z Yang, A Hackshaw, Q Feng, X Fu… - … journal of cancer, 2017 - Wiley Online Library
Gefitinib, erlotinib and afatinib are three widely used epidermal growth factor receptor
tyrosine kinase inhibitors (EGFR TKIs) for treating advanced non‐small cell lung cancer …

Practical guidelines for therapeutic drug monitoring of anticancer tyrosine kinase inhibitors: focus on the pharmacokinetic targets

H Yu, N Steeghs, CM Nijenhuis, JHM Schellens… - Clinical …, 2014 - Springer
There is accumulating evidence for potential benefits of therapeutic drug monitoring (TDM)
in the treatment of cancer with tyrosine kinase inhibitors (TKIs). Relationships between …

[HTML][HTML] Compound EGFR mutations and response to EGFR tyrosine kinase inhibitors

S Kobayashi, HM Canepa, AS Bailey… - Journal of Thoracic …, 2013 - Elsevier
Background: Non–small-cell lung cancers (NSCLCs) containing EGFR mutations are
exquisitely sensitive to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors …

Determining the optimal dose in the development of anticancer agents

RHJ Mathijssen, A Sparreboom, J Verweij - Nature reviews Clinical …, 2014 - nature.com
Identification of the optimal dose remains a key challenge in drug development. For cytotoxic
drugs, the standard approach is based on identifying the maximum tolerated dose (MTD) in …