Understanding and targeting resistance mechanisms in NSCLC

J Rotow, TG Bivona - Nature Reviews Cancer, 2017 - nature.com
The expanding spectrum of both established and candidate oncogenic driver mutations
identified in non-small-cell lung cancer (NSCLC), coupled with the increasing number of …

MET-dependent solid tumours—molecular diagnosis and targeted therapy

R Guo, J Luo, J Chang, N Rekhtman, M Arcila… - Nature reviews Clinical …, 2020 - nature.com
Attempts to develop MET-targeted therapies have historically focused on MET-expressing
cancers, with limited success. Thus, MET expression in the absence of a genomic marker of …

Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

L Goyal, SK Saha, LY Liu, G Siravegna, I Leshchiner… - Cancer discovery, 2017 - AACR
Genetic alterations in the fibroblast growth factor receptor (FGFR) pathway are promising
therapeutic targets in many cancers, including intrahepatic cholangiocarcinoma (ICC). The …

Molecular mechanisms of acquired resistance to MET tyrosine kinase inhibitors in patients with MET exon 14–mutant NSCLC

G Recondo, M Bahcall, LF Spurr, J Che, B Ricciuti… - Clinical Cancer …, 2020 - AACR
Purpose: Molecular mechanisms of acquired resistance to MET tyrosine kinase inhibitors
(TKI) are poorly understood. We aimed to characterize the genomic mechanisms of …

Targeting MET Dysregulation in Cancer

G Recondo, J Che, PA Jänne, MM Awad - Cancer discovery, 2020 - AACR
Aberrant MET signaling can drive tumorigenesis in several cancer types through a variety of
molecular mechanisms including MET gene amplification, mutation, rearrangement, and …

Capmatinib (INC280) is active against models of non–small cell lung cancer and other cancer types with defined mechanisms of MET activation

S Baltschukat, BS Engstler, A Huang, HX Hao… - Clinical Cancer …, 2019 - AACR
Purpose: The selective MET inhibitor capmatinib is being investigated in multiple clinical
trials, both as a single agent and in combination. Here, we describe the preclinical data of …

[HTML][HTML] Sensitivity and resistance of MET exon 14 mutations in lung cancer to eight MET tyrosine kinase inhibitors in vitro

T Fujino, Y Kobayashi, K Suda, T Koga… - Journal of Thoracic …, 2019 - Elsevier
Background MNNG HOS transforming gene (MET) exon 14 mutations in lung cancer,
including exon 14 skipping and point mutations, have been attracting the attention of …

[HTML][HTML] The race to target MET exon 14 skipping alterations in non-small cell lung cancer: the why, the how, the who, the unknown, and the inevitable

T Reungwetwattana, Y Liang, V Zhu, SHI Ou - Lung cancer, 2017 - Elsevier
A number of small molecule tyrosine kinase inhibitors (TKIs) have now been approved for
the treatment of non-small cell lung cancers (NSCLC), including those targeted against …

Targeting receptor tyrosine kinase MET in cancer: small molecule inhibitors and clinical progress

JJ Cui - Journal of medicinal chemistry, 2014 - ACS Publications
The HGF/MET signaling pathway is critical in mediating a wide range of normal
physiological functions including embryological development, wound healing, and tissue …

[HTML][HTML] Acquired resistance to crizotinib in NSCLC with MET exon 14 skipping

RS Heist, LV Sequist, D Borger, JF Gainor… - Journal of Thoracic …, 2016 - Elsevier
Introduction MET proto-oncogene, receptor tyrosine kinase gene (MET) exon 14 skipping is
a targetable alteration in lung cancer. Treatment with MET proto-oncogene, receptor tyrosine …