The impact of multiple low-level BCR-ABL1 mutations on response to ponatinib

WT Parker, DTO Yeung, AL Yeoman… - Blood, The Journal …, 2016 - ashpublications.org
The third-generation tyrosine kinase inhibitor (TKI) ponatinib shows activity against all
common BCR-ABL1 single mutants, including the highly resistant BCR-ABL1-T315I mutant …

Compound mutations in BCR-ABL1 are not major drivers of primary or secondary resistance to ponatinib in CP-CML patients

MW Deininger, JG Hodgson, NP Shah… - Blood, The Journal …, 2016 - ashpublications.org
BCR-ABL1 kinase domain mutations can confer resistance to first-and second-generation
tyrosine kinase inhibitors (TKIs) in chronic myeloid leukemia (CML). In preclinical studies …

[HTML][HTML] Comprehensive analysis of the in vitro potency of ponatinib, and all other approved BCR-ABL tyrosine kinase inhibitors (TKIs), against a panel of single and …

JM Gozgit, A Schrock, TH Chen, T Clackson, VM Rivera - Blood, 2013 - Elsevier
Background Secondary mutations in BCR-ABL are the most common cause of resistance to
TKIs in patients (pts) with chronic myeloid leukemia (CML). Ponatinib is a potent pan-BCR …

[HTML][HTML] Ponatinib in patients (pts) with chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) resistant or …

JE Cortes, DW Kim, J Pinilla-Ibarz, PD le Coutre… - Blood, 2013 - Elsevier
Background Ponatinib is a potent, oral, pan-BCR-ABL inhibitor with activity against native
and mutant forms of BCR-ABL, including the tyrosine kinase inhibitor (TKI)-resistant T315I …

[HTML][HTML] BCR-ABL1 compound mutants display differential and dose-dependent responses to ponatinib

K Byrgazov, CB Lucini, P Valent, O Hantschel… - …, 2018 - ncbi.nlm.nih.gov
The third-generation tyrosine kinase inhibitor (TKI) ponatinib exerts a strong anti-neoplastic
effect in all stages of chronic myeloid leukemia (CML) as well as in Philadelphia (Ph) …

A phase 2 trial of ponatinib in Philadelphia chromosome–positive leukemias

JE Cortes, DW Kim, J Pinilla-Ibarz… - … England Journal of …, 2013 - Mass Medical Soc
Background Ponatinib is a potent oral tyrosine kinase inhibitor of unmutated and mutated
BCR-ABL, including BCR-ABL with the tyrosine kinase inhibitor–refractory threonine-to …

[HTML][HTML] All tyrosine kinase inhibitor-resistant chronic myelogenous cells are highly sensitive to ponatinib

O Cassuto, M Dufies, A Jacquel, G Robert, C Ginet… - Oncotarget, 2012 - ncbi.nlm.nih.gov
The advent of tyrosine kinase inhibitor (TKI) therapy has considerably improved the survival
of patients suffering chronic myelogenous leukemia (CML). Indeed, inhibition of BCR-ABL …

[HTML][HTML] Efficacy and safety of ponatinib in patients with accelerated phase or blast phase chronic myeloid leukemia (AP-CML or BP-CML) or Philadelphia …

HM Kantarjian, DW Kim, J Pinilla-Ibarz, P le Coutre… - Blood, 2012 - Elsevier
Abstract Abstract 915 Background: Many patients (pts) with advanced Ph+ leukemias
experience failure of all currently available tyrosine kinase inhibitors (TKIs) targeting BCR …

Potential of ponatinib to treat chronic myeloid leukemia and acute lymphoblastic leukemia

KE Price, N Saleem, G Lee… - OncoTargets and therapy, 2013 - Taylor & Francis
Development of BCR-ABL tyrosine kinase inhibitors (TKIs) have improved outcomes for
patients diagnosed with chronic myeloid leukemia and Philadelphia chromosome positive …

[HTML][HTML] A pivotal phase 2 trial of ponatinib in patients with chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia …

JE Cortes, DW Kim, J Pinilla-Ibarz, P le Coutre… - Blood, 2012 - Elsevier
Abstract Abstract 163 Background: Despite progress in Ph+ leukemia therapy, patients who
experience failure of tyrosine kinase inhibitors (TKIs) and those with the T315I BCR-ABL …