Clinical pharmacokinetics of the BCR–ABL tyrosine kinase inhibitor nilotinib
C Tanaka, OQP Yin, V Sethuraman… - Clinical …, 2010 - Wiley Online Library
… to imatinib in blocking proliferation of BCR–ABL-dependent CML cell lines. Nilotinib inhibits
BCR–ABL … cell lines containing BCR–ABL point mutants commonly seen in patients with …
BCR–ABL … cell lines containing BCR–ABL point mutants commonly seen in patients with …
Nilotinib: optimal therapy for patients with chronic myeloid leukemia and resistance or intolerance to imatinib
R Swords, D Mahalingam… - Drug design …, 2009 - Taylor & Francis
… This led to the development of nilotinib, a high affinity … of imatinib and nilotinib with BCR-ABL.
The reduced requirement for hydrogen bonding with nilotinib compared to imatinib, allows …
The reduced requirement for hydrogen bonding with nilotinib compared to imatinib, allows …
Long-term outcomes with frontline nilotinib versus imatinib in newly diagnosed chronic myeloid leukemia in chronic phase: ENESTnd 10-year analysis
HM Kantarjian, TP Hughes, RA Larson, DW Kim… - Leukemia, 2021 - nature.com
… BCR-ABL1 IS > 10% at 3 months; moreover, more patients in … nilotinib arms versus the imatinib
arm achieved BCR-ABL1 IS … BCR-ABL1 IS ≤ 10% at 3 months was higher in the nilotinib …
arm achieved BCR-ABL1 IS … BCR-ABL1 IS ≤ 10% at 3 months was higher in the nilotinib …
Enhanced BCR-ABL kinase inhibition does not result in increased inhibition of downstream signaling pathways or increased growth suppression in CML progenitors
H Konig, M Holtz, H Modi, P Manley, TL Holyoake… - Leukemia, 2008 - nature.com
… nilotinib, a more potent BCR-ABL … nilotinib and imatinib on BCR-ABL TK activity. Although
the maximal inhibition of CRKL phosphorylation by nilotinib and imatinib was similar, nilotinib …
the maximal inhibition of CRKL phosphorylation by nilotinib and imatinib was similar, nilotinib …
Imatinib and nilotinib induce apoptosis of chronic myeloid leukemia cells through a Bim-dependant pathway modulated by cytokines
F Belloc, F Moreau-Gaudry, M Uhalde… - Cancer biology & …, 2007 - Taylor & Francis
… , imatinib is not completely specific for BCR-ABL … of BCR-ABL tyrosine kinase, nilotinib.We
demonstrate that inhibition of BCR-ABL auto-phosphorylation by either imatinib or nilotinib …
demonstrate that inhibition of BCR-ABL auto-phosphorylation by either imatinib or nilotinib …
The BCR-ABL1 inhibitors imatinib and ponatinib decrease plasma cholesterol and atherosclerosis, and nilotinib and ponatinib activate coagulation in a translational …
… various BCR-ABL inhibitors, we demonstrate that first, second and third generation BCR-ABL …
The first-generation inhibitor imatinib was proven safe, with evident benefit for plasma lipid …
The first-generation inhibitor imatinib was proven safe, with evident benefit for plasma lipid …
Nilotinib
GL Plosker, DM Robinson - Drugs, 2008 - Springer
… BCR-ABL protein in a similar manner to imatinib, although nilotinib has a higher binding
affinity and ● In the phase I study, which involved administraselectivity for the ABL kinase.[5,12,…
affinity and ● In the phase I study, which involved administraselectivity for the ABL kinase.[5,12,…
Nilotinib significantly induces apoptosis in imatinib resistant K562 cells with wild-type BCR–ABL, as effectively as in parental sensitive counterparts
… Nilotinib is more effective in this respect than imatinib. We have shown that nilotinib induces
apoptosis in imatinib-resistant K562 CML cells which have the wild-type BCR– ABL fusion …
apoptosis in imatinib-resistant K562 CML cells which have the wild-type BCR– ABL fusion …
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
… many imatinib mesylate–resistant BCR-ABL kinase … BCR-ABL cells to compare incidence
and types of KD mutants emerging in the presence of imatinib mesylate, dasatinib, and nilotinib…
and types of KD mutants emerging in the presence of imatinib mesylate, dasatinib, and nilotinib…
Imatinib and Nilotinib inhibit Bcr–Abl-induced ROS through targeted degradation of the NADPH oxidase subunit p22phox
WD Landry, JF Woolley, TG Cotter - Leukemia research, 2013 - Elsevier
… inhibition of Bcr–Abl signalling, by either Imatinib or Nilotinib, … a possible link between
Bcr–Abl signalling and ROS production … associated with Imatinib and Nilotinib treatment in CML. …
Bcr–Abl signalling and ROS production … associated with Imatinib and Nilotinib treatment in CML. …