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Joseph C. Alvarnas, Patrick A. Brown, Patricia Aoun, Karen Kuhn Ballen, Stefan K. Barta, Uma Borate, Michael W. Boyer, Patrick W. Burke, Ryan Cassaday, Januario E. Castro, Peter F. Coccia, Steven E. Coutre, Lloyd E. Damon, Daniel J. DeAngelo, Dan Douer, Olga Frankfurt, John P. Greer, Robert A. Johnson, Hagop M. Kantarjian, Rebecca B. Klisovic, Gary Kupfer, Mark Litzow, Arthur Liu, Arati V. Rao, Bijal Shah, Geoffrey L. Uy, Eunice S. Wang, Andrew D. Zelenetz, Kristina Gregory and Courtney Smith

, EPOR, JAK2, PDGFR β, EBF1, FLT2, IL7R , and SH2B3 genes. 44 – 46 A recent publication found kinase-activating alternations in 91% of Ph-like ALL cases. 47 Therefore, use of the ABL1 tyrosine kinase inhibitor (TKI) imatinib or other targeted

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Aparna Parikh, Chloe Atreya, W. Michael Korn and Alan P. Venook

trastuzumab and lapatinib. 9 , 19 Single-agent trastuzumab did not markedly affect HER2 and EGFR phosphorylation but produced dose-dependent suppression of HER3 activation. The addition of lapatinib, a tyrosine kinase inhibitor (TKI) that targets HER2 and

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Presenter : Gregory J. Riely

, said Dr. Riely. Treating EGFR -Mutated NSCLC “ EGFR -sensitizing mutations are the molecular subtype we've known about and have been treating the longest,” he said. Multiple randomized trials have shown that EGFR tyrosine kinase inhibitors (TKIs) are

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Patrick A. Brown, Matthew Wieduwilt, Aaron Logan, Daniel J. DeAngelo, Eunice S. Wang, Amir Fathi, Ryan D. Cassaday, Mark Litzow, Anjali Advani, Patricia Aoun, Bhavana Bhatnagar, Michael W. Boyer, Teresa Bryan, Patrick W. Burke, Peter F. Coccia, Steven E. Coutre, Nitin Jain, Suzanne Kirby, Arthur Liu, Stephanie Massaro, Ryan J. Mattison, Olalekan Oluwole, Nikolaos Papadantonakis, Jae Park, Jeffrey E. Rubnitz, Geoffrey L. Uy, Kristina M. Gregory, Ndiya Ogba and Bijal Shah

, however, the difference in overall survival (OS) and outcomes between older and younger patients is less than with Ph-negative ALL, due in part to the availability of well-tolerated, effective oral BCR-ABL1 tyrosine kinase inhibitor (TKI) therapy. 4 – 10

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Elizabeth R. Plimack and Gary R. Hudes

other factors. Sunitinib, an oral tyrosine kinase inhibitor (TKI), is the agent most familiar to clinicians because it has been in clinical use the longest. The “4 + 2” schedule of sunitinib (4 weeks on, 2 weeks off) at a starting dose of 50 mg daily is

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David D. Stenehjem, Frederick Albright, Kuan-Ling Kuo, Karina Raimundo, Hillevi Bauer, Paul J. Shami, Michael W. Deininger, Lei Chen and Diana I. Brixner

to imatinib. 5 The second-generation tyrosine kinase inhibitors (TKIs) dasatinib and nilotinib have increased potency compared with imatinib. 6 , 7 They were approved initially for patients in whom imatinib had failed, and subsequently for front

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Ralph M. Turner, PhD b From a AstraZeneca Pharmaceuticals, LP, and b HealthCore, Inc. Background : The benefit of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) therapies over standard chemotherapy among patients diagnosed

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George D. Demetri, Robert S. Benjamin, Charles D. Blanke, Jean-Yves Blay, Paolo Casali, Haesun Choi, Christopher L. Corless, Maria Debiec-Rychter, Ronald P. DeMatteo, David S. Ettinger, George A. Fisher, Christopher D. M. Fletcher, Alessandro Gronchi, Peter Hohenberger, Miranda Hughes, Heikki Joensuu, Ian Judson, Axel Le Cesne, Robert G. Maki, Michael Morse, Alberto S. Pappo, Peter W. T. Pisters, Chandrajit P. Raut, Peter Reichardt, Douglas S. Tyler, Annick D. Van den Abbeele, Margaret von Mehren, Jeffrey D. Wayne and John Zalcberg

Sunitinib malate (SU011248, Sutent) is an oral TKI that is less specific than imatinib mesylate. In addition to inhibiting KIT and PDGFR, sunitinib acts on vascular endothelial growth factor receptors (VEGFR13), Fms-like tyrosine kinase-3, colony

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Suzanne George

Therapy Updates Pazopanib as a multitargeted tyrosine kinase inhibitor (TKI) has been included in the NCCN Guidelines for several years. Its inclusion is based on the randomized phase III PALETTE trial comparing pazopanib versus placebo in patients with

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Yong Li, Xian Chen, Yanchun Qu, Jia-Ming Fan, Yan Li, Hui Peng, Yaojie Zheng, Yihong Zhang and Hai-Bo Zhang

development of ROS1 inhibitors, including crizotinib and ceritinib. Crizotinib is a small molecule tyrosine kinase inhibitor (TKI) that was found to actively inhibit ALK , MET , and ROS1. Crizotinib was originally developed as an anti- MET molecule, 19