Tepotinib in Non–Small-Cell Lung Cancer with <i>MET</i> Exon 14 Skipping Mutations

Paik, Paul K.; Felip, Enriqueta; Veillon, Rémi; Sakai, Hiroshi; Cortot, A.; Garassino, Marina Chiara; Mazières, Julien; Viteri, Santiago; Senellart, Hélène; Meerbeeck, Jan Van; Raskin, Jo; Reinmuth, Niels; Conté, Pierfranco; Kowalski, Dariusz M.; Cho, Byoung Chul; Patel, Jyoti D.; Horn, Leora; Griesinger, Frank; Han, Ji Youn; Kim, Young Chul; Chang, Gee Chen; Tsai, Chia‐Lin; Yang, James Chih‐Hsin; Chen, Yuh Min; Smit, Egbert F.; Wekken, Anthonie J. van der; Kato, Terufumi; Juraeva, Dilafruz; Stroh, Christopher; Bruns, Rolf; Straub, Josef; Johne, Andreas; Scheele, J.; Heymach, John V.; Le, Xiuning

doi:10.1056/nejmoa2004407

Cited by 572 publications

(615 citation statements)

References 38 publications

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“…In a phase III study of tivantinib in patients with NSCLC, tivantinib combined with erlotinib led to a significant prolongation of PFS (13.0 vs. 7.5 months) and OS (25.5 vs. 20.3 months) compared to erlotinib monotherapy (Scagliotti et al, 2018). A phase II study evaluated the efficacy of tepotinib in patients with advanced NSCLC with METex14 alterations (Paik et al, 2020). The response rate of the liquid-biopsy group (n = 66) and the tissue-biopsy group (n = 60) were 48% and 50%, respectively.…”

Section: Hgf/c-met Signaling In Non-digestive System Cancermentioning

confidence: 99%

HGF/c-Met Axis: The Advanced Development in Digestive System Cancer

Shao

Pan

et al. 2020

Front. Cell Dev. Biol.

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Numerous studies have indicated that abnormal activation of the HGF/c-Met signaling pathway can lead to cell proliferation, invasiveness, and metastasis of cancers of the digestive system. Moreover, overexpression of c-Met has been implicated in poor prognosis of patients with these forms of cancer, suggesting the possibility for HGF/c-Met axis as a potential therapeutic target. Despite the large number of clinical and preclinical trials worldwide, no significant positive success in the use of anti-HGF/c-Met treatments on cancers of the digestive system has been achieved. In this review, we summarize advanced development of clinical research on HGF/c-Met antibody and small-molecule c-Met inhibitors of cancers of the digestive system and provide a possible direction for future research.

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Section: Hgf/c-met Signaling In Non-digestive System Cancermentioning

confidence: 99%

HGF/c-Met Axis: The Advanced Development in Digestive System Cancer

Shao

Pan

et al. 2020

Front. Cell Dev. Biol.

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“…Both of these adverse events were thought to be unrelated to this drug combination, but the potential toxicities of such drug combinations will need to be studied in future prospective cohorts of patients with appropriate performance status and comorbidities. Lastly, we are hopeful that the use of newer, more specific MET inhibitors including capmatinib 7,20 (which is FDA approved) and tepotinib 21 in combination with selpercatinib may result in increased efficacy and better tolerability of this drug combination.…”

Section: Discussionmentioning

confidence: 99%

Overcoming MET-Dependent Resistance to Selective RET Inhibition in Patients with RET Fusion–Positive Lung Cancer by Combining Selpercatinib with Crizotinib

Rosen

Johnson

Clifford

et al. 2021

Clinical Cancer Research

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and Company. L.M.S. reports consulting fees from EMD Serono, scientific advisory board roles for Loxo Oncology and Foghorn Therapeutics, and honorarium from Astra Zeneca. B.S.T. reports honoraria and research funding from Genentech and discovery board activities for Boehringer Ingelheim and Loxo Oncology; all stated activities were outside of the work described herein. M. Ladanyi reports ad hoc advisory board roles for

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“…Cabozantinib (multi-TKI), tepotinib (MET-selective TKI), glesatinib (multi-TKI) and savolitinib (MET-selective TKI) are other MET inhibitors that are under research in clinical trials [ 233 , 234 ].…”

Section: Tyrosine Kinase Receptor Inhibitors Developed For Cancer mentioning

confidence: 99%

Tyrosine Kinase Receptors in Oncology

Esteban-Villarrubia

Castillo

Pozas

et al. 2020

IJMS

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Tyrosine kinase receptors (TKR) comprise more than 60 molecules that play an essential role in the molecular pathways, leading to cell survival and differentiation. Consequently, genetic alterations of TKRs may lead to tumorigenesis and, therefore, cancer development. The discovery and improvement of tyrosine kinase inhibitors (TKI) against TKRs have entailed an important step in the knowledge-expansion of tumor physiopathology as well as an improvement in the cancer treatment based on molecular alterations over many tumor types. The purpose of this review is to provide a comprehensive review of the different families of TKRs and their role in the expansion of tumor cells and how TKIs can stop these pathways to tumorigenesis, in combination or not with other therapies. The increasing growth of this landscape is driving us to strengthen the development of precision oncology with clinical trials based on molecular-based therapy over a histology-based one, with promising preliminary results.

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Tepotinib in Non–Small-Cell Lung Cancer with MET Exon 14 Skipping Mutations

Cited by 572 publications

References 38 publications

HGF/c-Met Axis: The Advanced Development in Digestive System Cancer

HGF/c-Met Axis: The Advanced Development in Digestive System Cancer

Overcoming MET-Dependent Resistance to Selective RET Inhibition in Patients with RET Fusion–Positive Lung Cancer by Combining Selpercatinib with Crizotinib

Tyrosine Kinase Receptors in Oncology

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