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Susan O'Brien, Ellin Berman, Joseph O. Moore, Javier Pinilla-Ibarz, Jerald P. Radich, Paul J. Shami, B. Douglas Smith, David S. Snyder, Hema M. Sundar, Moshe Talpaz and Meir Wetzler

diagnosed CML. Dasatinib Dasatinib is a potent, orally available ABL kinase inhibitor. It binds to both the active and inactive conformation of the ABL kinase domain and has in vitro activity against nearly all imatinib-resistant BCR-ABL mutations except

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Paul J. Shami

, nilotinib, and dasatinib, based on a review Describe the case for the use of imatinib in first-line therapy of CML, based on a review Describe the case for the use of dasatinib or nilotinib in first-line therapy of CML, based on a review

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Stephen Harnicar

intolerance, dasatinib (Sprycel) and nilotinib (Tasigna) can now be used in front-line therapy because of results of 2 different trials. Dasatinib was compared with imatinib first-line and after a minimum follow-up of 12 months; the rates of confirmed CCyR

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Susan O'Brien, Camille N. Abboud, Mojtaba Akhtari, Jessica Altman, Ellin Berman, Daniel J. DeAngelo, Steven Devine, Amir T. Fathi, Jason Gotlib, Madan Jagasia, Joseph O. Moore, Javier Pinilla-Ibarz, Jerald P. Radich, Vishnu V.B. Reddy, Neil P. Shah, Paul J. Shami, B. Douglas Smith, David S. Snyder, Meir Wetzler and Furhan Yunus

rates than those receiving standard-dose imatinib. High-dose imatinib currently has only a limited role in first-line therapy. Dasatinib Dasatinib is a potent, orally available ABL kinase inhibitor, similar to imatinib but with the added

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Susan O'Brien, Ellin Berman, Hossein Borghaei, Daniel J. DeAngelo, Marcel P. Devetten, Steven Devine, Harry P. Erba, Jason Gotlib, Madan Jagasia, Joseph O. Moore, Tariq Mughal, Javier Pinilla-Ibarz, Jerald P. Radich, Neil P. Shah, Paul J. Shami, B. Douglas Smith, David S. Snyder, Martin S. Tallman, Moshe Talpaz and Meir Wetzler

imatinib resistance with a novel ABL kinase inhibitor . Science 2004 ; 305 : 399 – 401 . 22 Talpaz M Shah NP Kantarjian H . Dasatinib in imatinib resistant Philadelphia chromosome-positive leukemias . N Eng J Med 2006 ; 354 : 2531 – 2541

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Scott M. Lindhorst, Richard D. Lopez and Ronald D. Sanders

newly diagnosed CML are noted to experience a 40% to 70% rate of major molecular response (BCR/ABL transcript level <0.1%). 5 The more potent second-generation TKIs (ie, nilotinib and dasatinib) produce higher molecular response rates than imatinib

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Ellin Berman

Resistance to Front-Line Therapy: How Big is the Problem? Ponatinib was fast-tracked by the FDA in December 2012, for use in patients whose disease progressed on or who could not tolerate therapy with first-line agents imatinib, dasatinib, or

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Jerald P. Radich

include imatinib, nilotinib, and dasatinib. 2 - 5 These second-generation agents tend to be preferred over higher doses of imatinib, as that approach is more toxic, explained Dr. Radich. The data supporting imatinib for chronic-phase CML came from the

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Susan O’Brien, Jerald P. Radich, Camille N. Abboud, Mojtaba Akhtari, Jessica K. Altman, Ellin Berman, Daniel J. DeAngelo, Michael Deininger, Steven Devine, Amir T. Fathi, Jason Gotlib, Madan Jagasia, Patricia Kropf, Joseph O. Moore, Arnel Pallera, Javier Pinilla-Ibarz, Vishnu VB. Reddy, Neil P. Shah, B. Douglas Smith, David S. Snyder, Meir Wetzler, Kristina Gregory and Hema Sundar

) therapy (with imatinib, dasatinib, or nilotinib) is the standard first-line treatment for patients with newly diagnosed chronic-phase CML (see CML-1, page 1329). 3 - 5 Early molecular response to first-line TKI therapy is emerging as an effective

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Matthew P. Banegas, Donna R. Rivera, Maureen C. O’Keeffe-Rosetti, Nikki M. Carroll, Pamala A. Pawloski, David C. Tabano, Mara M. Epstein, Kai Yeung, Mark C. Hornbrook, Christine Lu and Debra P. Ritzwoller

, or acquired, resistance (developing during imatinib treatment). 4 To overcome mutational resistance, 3 second-generation oral TKIs—dasatinib, nilotinib, and bosutinib—and 1 third-generation oral TKI, ponatinib, have received approval for use as first