Impact of Baseline BCR-ABL Mutations on Response to Nilotinib in Patients With Chronic Myeloid Leukemia in Chronic Phase
Purpose Nilotinib is a second-generation tyrosine kinase inhibitor indicated for the treatment
of patients with chronic myeloid leukemia (CML) in chronic phase (CP; CML-CP) and …
of patients with chronic myeloid leukemia (CML) in chronic phase (CP; CML-CP) and …
Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is effective in patients with Philadelphia chromosome–positive chronic …
HM Kantarjian, F Giles, N Gattermann… - Blood, The Journal …, 2007 - ashpublications.org
Nilotinib, an orally bioavailable, selective Bcr-Abl tyrosine kinase inhibitor, is 30-fold more
potent than imatinib in pre-clinical models, and overcomes most imatinib resistant BCR-ABL …
potent than imatinib in pre-clinical models, and overcomes most imatinib resistant BCR-ABL …
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance
T O'Hare, WC Shakespeare, X Zhu, CA Eide… - Cancer cell, 2009 - cell.com
Inhibition of BCR-ABL by imatinib induces durable responses in many patients with chronic
myeloid leukemia (CML), but resistance attributable to kinase domain mutations can lead to …
myeloid leukemia (CML), but resistance attributable to kinase domain mutations can lead to …
Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)–based mutagenesis screen: high efficacy of …
HA Bradeen, CA Eide, T O'Hare, KJ Johnson, SG Willis… - Blood, 2006 - ashpublications.org
Abstract BMS-354825 (dasatinib) and AMN107 (nilotinib) are potent alternate Abl inhibitors
with activity against many imatinib mesylate–resistant BCR-ABL kinase domain (KD) …
with activity against many imatinib mesylate–resistant BCR-ABL kinase domain (KD) …
Nilotinib is associated with a reduced incidence of BCR-ABL mutations vs imatinib in patients with newly diagnosed chronic myeloid leukemia in chronic phase
A Hochhaus, G Saglio, RA Larson… - Blood, The Journal …, 2013 - ashpublications.org
In patients with chronic myeloid leukemia, BCR-ABL mutations contribute to resistance to
tyrosine kinase inhibitor therapy. We examined the occurrence of treatment-emergent …
tyrosine kinase inhibitor therapy. We examined the occurrence of treatment-emergent …
[HTML][HTML] ABL001, a potent allosteric inhibitor of BCR-ABL, prevents emergence of resistant disease when administered in combination with nilotinib in an in vivo …
A Wylie, J Schoepfer, G Berellini, H Cai, G Caravatti… - Blood, 2014 - Elsevier
Background: Chronic myelogenous leukemia (CML) and a subset of acute lymphoblastic
leukemia (ALL) are caused by the t (9; 22)(q34; q11. 2) chromosome translocation, resulting …
leukemia (ALL) are caused by the t (9; 22)(q34; q11. 2) chromosome translocation, resulting …
Impact of BCR-ABL mutations on patients with chronic myeloid leukemia
A Hochhaus, PL Rosée, MC Müller, T Ernst… - Cell cycle, 2011 - Taylor & Francis
Therapies that target BCR-ABL in chronic myeloid leukemia, including imatinib, dasatinib
and nilotinib, have dramatically improved patient outcome. BCR-ABL mutations, however …
and nilotinib, have dramatically improved patient outcome. BCR-ABL mutations, however …
SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib
T O'Hare, CA Eide, JW Tyner… - Proceedings of the …, 2008 - National Acad Sciences
Imatinib inhibits Bcr-Abl, the oncogenic tyrosine kinase that causes chronic myeloid
leukemia. The second-line inhibitors nilotinib and dasatinib are effective in patients with …
leukemia. The second-line inhibitors nilotinib and dasatinib are effective in patients with …
Poor response to second-line kinase inhibitors in chronic myeloid leukemia patients with multiple low-level mutations, irrespective of their resistance profile
Specific imatinib-resistant BCR-ABL1 mutations (Y253H, E255K/V, T315I, F317L, and
F359V/C) predict failure of second-line nilotinib or dasatinib therapy in patients with chronic …
F359V/C) predict failure of second-line nilotinib or dasatinib therapy in patients with chronic …
[HTML][HTML] Nilotinib Is Highly Active and Safe in Chronic Phase Chronic Myelogenous Leukemia (CML-CP) Patients with Imatinib-Resistance or Intolerance.
HM Kantarjian, A Hochhaus, J Cortes, G Martinelli… - Blood, 2007 - Elsevier
Background: Nilotinib is a novel, selective BCR-ABL inhibitor, designed to bind the ATP-
binding site of BCR-ABL protein with higher affinity than imatinib. It is more potent than …
binding site of BCR-ABL protein with higher affinity than imatinib. It is more potent than …