The resistance to EGFR-TKIs in non-small cell lung cancer: from molecular mechanisms to clinical application of new therapeutic strategies

C Laface, FM Maselli, AN Santoro, ML Iaia, F Ambrogio… - Pharmaceutics, 2023 - mdpi.com
Almost 17% of Western patients affected by non-small cell lung cancer (NSCLC) have an
activating epidermal growth factor receptor (EGFR) gene mutation. Del19 and L858R are the …

Candidate mechanisms of acquired resistance to first-line osimertinib in EGFR-mutated advanced non-small cell lung cancer

J Chmielecki, JE Gray, Y Cheng, Y Ohe… - Nature …, 2023 - nature.com
Osimertinib, an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI),
potently and selectively inhibits EGFR-TKI-sensitizing and EGFR T790M resistance …

Structure–activity relationship studies based on quinazoline derivatives as EGFR kinase inhibitors (2017–present)

A Șandor, I Ionuț, G Marc, I Oniga, D Eniu, O Oniga - Pharmaceuticals, 2023 - mdpi.com
The epidermal growth factor receptor (EGFR) plays a critical role in the tumorigenesis of
various forms of cancer. Targeting the mutant forms of EGFR has been identified as an …

Analysis of acquired resistance mechanisms to osimertinib in patients with EGFR-mutated advanced non-small cell lung cancer from the AURA3 trial

J Chmielecki, T Mok, YL Wu, JY Han, MJ Ahn… - Nature …, 2023 - nature.com
Osimertinib, an epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI),
potently and selectively inhibits EGFR-TKI-sensitizing and EGFR T790M resistance …

Befotertinib (D-0316) versus icotinib as first-line therapy for patients with EGFR-mutated locally advanced or metastatic non-small-cell lung cancer: a multicentre, open …

S Lu, J Zhou, H Jian, L Wu, Y Cheng, Y Fan… - The Lancet …, 2023 - thelancet.com
Summary Background Befotertinib (D-0316) is a novel, selective oral third-generation
epidermal growth factor receptor (EGFR) tyrosine-kinase inhibitor. This phase 3 trial …

Precision oncology comes of age: designing best-in-class small molecules by integrating two decades of advances in chemistry, target biology, and data science

DD Stuart, A Guzman-Perez, N Brooijmans… - Cancer Discovery, 2023 - AACR
Small-molecule drugs have enabled the practice of precision oncology for genetically
defined patient populations since the first approval of imatinib in 2001. Scientific and …

Design, synthesis, anticancer evaluation, and in silico studies of some thieno[2,3‐d]pyrimidine derivatives as EGFR inhibitors

MTM Sayed, PA Halim, AK El‐Ansary… - Drug Development …, 2023 - Wiley Online Library
Abstract New series of 20 thieno [2, 3‐d] pyrimidine derivatives have been synthesized. The
National Cancer Institute evaluated all the newly synthesized compounds for their …

Cucurbitacin I reverses tumor-associated macrophage polarization to affect cancer cell metastasis

X Gong, Y Liu, K Liang, Z Chen, K Ding, L Qiu… - International Journal of …, 2023 - mdpi.com
The tumor microenvironment plays a critical role in tumor progression and immune
regulation. As one of the most important components of the tumor microenvironment …

Real‐world treatment patterns of metastatic non‐small cell lung cancer patients receiving epidermal growth factor receptor tyrosine kinase inhibitors

R Shenolikar, S Liu, A Shah, J Tse, Y Cao… - Cancer …, 2023 - Wiley Online Library
Background Several epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKI)
have been approved for first‐line (1L) treatment of EGFR‐mutated metastatic non‐small cell …

The effect of EGFR‐TKIs on survival in advanced non‐small‐cell lung cancer with EGFR mutations: A real‐world study

X Yu, J Si, J Wei, Y Wang, Y Sun, J Jin… - Cancer …, 2023 - Wiley Online Library
Background Few large‐scale studies have been published using real‐world data related to
overall survival (OS) improvements in advanced epidermal growth factor receptor (EGFR) …