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Rociletinib (CO-1686)

Sandra Ortiz-Cuaran, Matthias Scheffler, Dennis Plenker, Llona Dahmen, Andreas H Scheel, Lynnette Fernandez-Cuesta, Lydia Meder, Christine M Lovly, Thorsten Persigehl, Sabine Merkelbach-Bruse, Marc Bos, Sebastian Michels, Rieke Fischer, Kerstin Albus, Katharina König, Hans-Ulrich Schildhaus, Jana Fassunke, Michaela A Ihle, Helen Pasternack, Carina Heydt, Christian Becker, Janine Altmüller, Hongbin Ji, Christian Müller, Alexandra Florin, Johannes M Heuckmann, Peter Nuernberg, Sascha Ansén, Lukas C Heukamp, Johannes Berg, William Pao, Martin Peifer, Reinhard Buettner, Jürgen Wolf, Roman K Thomas, Martin L Sos
PURPOSE: To identify novel mechanisms of resistance to third-generation EGFR inhibitors in patients with lung adenocarcinoma that progressed under therapy with either AZD9291 or rociletinib (CO-1686). EXPERIMENTAL DESIGN: We analyzed tumor biopsies from seven patients obtained before, during, and/or after treatment with AZD9291 or rociletinib (CO-1686). Targeted sequencing and FISH analyses were performed, and the relevance of candidate genes was functionally assessed in in vitro models...
June 1, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Chris Karlovich, Jonathan W Goldman, Jong-Mu Sun, Elaina Mann, Lecia V Sequist, Krzysztof Konopa, Wei Wen, Philipp Angenendt, Leora Horn, David Spigel, Jean-Charles Soria, Benjamin Solomon, D Ross Camidge, Shirish Gadgeel, Cloud Paweletz, Lin Wu, Sean Chien, Patrick O'Donnell, Shannon Matheny, Darrin Despain, Lindsey Rolfe, Mitch Raponi, Andrew R Allen, Keunchil Park, Heather Wakelee
PURPOSE: The evaluation of plasma testing for the EGFR resistance mutation T790M in NSCLC patients has not been broadly explored. We investigated the detection of EGFR activating and T790M mutations in matched tumor tissue and plasma, mostly from patients with acquired resistance to first-generation EGFR inhibitors. EXPERIMENTAL DESIGN: Samples were obtained from two studies, an observational study and a phase I trial of rociletinib, a mutant-selective inhibitor of EGFR that targets both activating mutations and T790M...
May 15, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Sai-Hong Ignatius Ou, Ross A Soo
EGFR tyrosine-kinase inhibitors (TKIs) have now been firmly established as the first-line treatment for non-small-cell lung cancer (NSCLC) patients harboring activating EGFR mutations, based on seven prospective randomized Phase III trials. However, despite significantly improved overall response rate and improved median progression-free survival when compared to platinum-doublet chemotherapy, EGFR-mutant NSCLC patients treated with EGFR TKIs invariably progress due to the emergence of acquired resistances, with the gatekeeper T790M mutation accounting for up to 60% of the resistance mechanisms...
2015: Drug Design, Development and Therapy
Lecia V Sequist, Jean-Charles Soria, Jonathan W Goldman, Heather A Wakelee, Shirish M Gadgeel, Andrea Varga, Vassiliki Papadimitrakopoulou, Benjamin J Solomon, Geoffrey R Oxnard, Rafal Dziadziuszko, Dara L Aisner, Robert C Doebele, Cathy Galasso, Edward B Garon, Rebecca S Heist, Jennifer Logan, Joel W Neal, Melody A Mendenhall, Suzanne Nichols, Zofia Piotrowska, Antoinette J Wozniak, Mitch Raponi, Chris A Karlovich, Sarah Jaw-Tsai, Jeffrey Isaacson, Darrin Despain, Shannon L Matheny, Lindsey Rolfe, Andrew R Allen, D Ross Camidge
BACKGROUND: Non-small-cell lung cancer (NSCLC) with a mutation in the gene encoding epidermal growth factor receptor (EGFR) is sensitive to approved EGFR inhibitors, but resistance develops, mediated by the T790M EGFR mutation in most cases. Rociletinib (CO-1686) is an EGFR inhibitor active in preclinical models of EGFR-mutated NSCLC with or without T790M. METHODS: In this phase 1-2 study, we administered rociletinib to patients with EGFR-mutated NSCLC who had disease progression during previous treatment with an existing EGFR inhibitor...
April 30, 2015: New England Journal of Medicine
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