Third-generation EGFR and ALK inhibitors: mechanisms of resistance and management

AJ Cooper, LV Sequist, JJ Lin - Nature Reviews Clinical Oncology, 2022 - nature.com
The discoveries of EGFR mutations and ALK rearrangements as actionable oncogenic
drivers in non-small-cell lung cancer (NSCLC) has propelled a biomarker-directed treatment …

Genetic markers in lung cancer diagnosis: a review

K Wadowska, I Bil-Lula, Ł Trembecki… - International journal of …, 2020 - mdpi.com
Lung cancer is the most often diagnosed cancer in the world and the most frequent cause of
cancer death. The prognosis for lung cancer is relatively poor and 75% of patients are …

[HTML][HTML] Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer

JC Soria, Y Ohe, J Vansteenkiste… - New England journal …, 2018 - Mass Medical Soc
Background Osimertinib is an oral, third-generation, irreversible epidermal growth factor
receptor tyrosine kinase inhibitor (EGFR-TKI) that selectively inhibits both EGFR-TKI …

Landscape of EGFR-Dependent and -Independent Resistance Mechanisms to Osimertinib and Continuation Therapy Beyond Progression in EGFR-Mutant NSCLC

X Le, S Puri, MV Negrao, MB Nilsson, J Robichaux… - Clinical Cancer …, 2018 - AACR
Purpose: Osimertinib was initially approved for T790M-positive non–small cell lung cancer
(NSCLC) and, more recently, for first-line treatment of EGFR-mutant NSCLC. However …

Investigating novel resistance mechanisms to third-generation EGFR tyrosine kinase inhibitor osimertinib in non–small cell lung cancer patients

Z Yang, N Yang, Q Ou, Y Xiang, T Jiang, X Wu… - Clinical Cancer …, 2018 - AACR
Purpose: The third-generation EGFR tyrosine kinase inhibitor osimertinib is approved to
treat patients with EGFR T790M-positive non–small cell lung cancer (NSCLC) who have …

EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research

RF Dong, ML Zhu, MM Liu, YT Xu, LL Yuan… - Pharmacological …, 2021 - Elsevier
With the development of precision medicine, molecular targeted therapy has been widely
used in the field of cancer, especially in non-small-cell lung cancer (NSCLC). Epidermal …

Acquired resistance to EGFR targeted therapy in non-small cell lung cancer: Mechanisms and therapeutic strategies

SM Lim, NL Syn, BC Cho, RA Soo - Cancer treatment reviews, 2018 - Elsevier
The tyrosine kinase inhibitors (TKIs) directed at sensitizing mutations in the epidermal
growth factor receptor (EGFR) gene represents a critical pillar in non-small cell lung cancer …

Third generation EGFR TKIs: current data and future directions

CS Tan, NB Kumarakulasinghe, YQ Huang, YLE Ang… - Molecular cancer, 2018 - Springer
Acquired T790 M mutation is the commonest cause of resistance for advanced non-small
cell lung cancer (NSCLC) epidermal growth factor receptor (EGFR) mutant patients who had …

The next tier of EGFR resistance mutations in lung cancer

HL Tumbrink, A Heimsoeth, ML Sos - Oncogene, 2021 - nature.com
EGFR mutations account for the majority of druggable targets in lung adenocarcinoma. Over
the past decades the optimization of EGFR inhibitors revolutionized the treatment options for …

Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC)

H Zhang, HY Zhao, XX Xi, YJ Liu, M Xin, S Mao… - European journal of …, 2020 - Elsevier
Epidermal growth factor receptor (EGFR), a member of the HER family, is closely related to
the development of multiple cancers. Herein, we report the discovery of small molecule …