Clinical pharmacokinetics of the BCRABL tyrosine kinase inhibitor nilotinib

C Tanaka, OQP Yin, V Sethuraman… - Clinical …, 2010 - Wiley Online Library
… to imatinib in blocking proliferation of BCRABL-dependent CML cell lines. Nilotinib inhibits
BCRABL … cell lines containing BCRABL 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 …

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

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-ABLnilotinib and imatinib on BCR-ABL TK activity. Although
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

The BCR-ABL1 inhibitors imatinib and ponatinib decrease plasma cholesterol and atherosclerosis, and nilotinib and ponatinib activate coagulation in a translational …

MG Pouwer, EJ Pieterman, L Verschuren… - Frontiers in …, 2018 - frontiersin.org
… 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 …

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,…

Nilotinib significantly induces apoptosis in imatinib resistant K562 cells with wild-type BCRABL, as effectively as in parental sensitive counterparts

HA Ekiz, G Can, U Gunduz, Y Baran - Hematology, 2010 - Taylor & Francis
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 BCRABL 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

Imatinib and Nilotinib inhibit BcrAbl-induced ROS through targeted degradation of the NADPH oxidase subunit p22phox

WD Landry, JF Woolley, TG Cotter - Leukemia research, 2013 - Elsevier
… inhibition of BcrAbl signalling, by either Imatinib or Nilotinib, … a possible link between
BcrAbl signalling and ROS production … associated with Imatinib and Nilotinib treatment in CML. …