Nilotinib: a phenylamino-pyrimidine derivative with activity against BCR-ABL, KIT and PDGFR kinases
A Quintás-Cardama, J Cortes - Future Oncology, 2008 - Taylor & Francis
… is a tyrosine kinase inhibitor 30-fold more potent than imatinib against BCR-ABL kinase.
Nilotinib is active against a wide range of imatinib-resistant BCR-ABL mutant isoforms, except …
Nilotinib is active against a wide range of imatinib-resistant BCR-ABL mutant isoforms, except …
Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib
O Hantschel, U Rix, G Superti-Furga - Leukemia & lymphoma, 2008 - Taylor & Francis
… of imatinib as … of imatinib-resistant mutations. Here, we review the current knowledge about
the target specificity of the two new inhibitors nilotinib and dasatinib in comparison to imatinib…
the target specificity of the two new inhibitors nilotinib and dasatinib in comparison to imatinib…
Nilotinib in imatinib-resistant or imatinib-intolerant patients with chronic myeloid leukemia in chronic phase: 48-month follow-up results of a phase II study
FJ Giles, PD Le Coutre, J Pinilla-Ibarz, RA Larson… - Leukemia, 2013 - nature.com
… Nilotinib (Tasigna; Novartis Pharmaceuticals) is a second-generation TKI that was … against
BCR–ABL1 mutations associated with resistance to imatinib. Compared with imatinib, nilotinib …
BCR–ABL1 mutations associated with resistance to imatinib. Compared with imatinib, nilotinib …
The ins and outs of bcr-abl inhibition
EP Reddy, AK Aggarwal - Genes & cancer, 2012 - journals.sagepub.com
… Note that imatinib and nilotinib bind the inactive state of Abl in a similar manner, including
a hydrogen bond with the main chain amide of interlobe residue Met318, a hydrogen bond …
a hydrogen bond with the main chain amide of interlobe residue Met318, a hydrogen bond …
Bcr-Abl resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107)
N Von Bubnoff, PW Manley, J Mestan, J Sanger… - Blood, 2006 - ashpublications.org
… Our findings suggest that nilotinib might be superior to imatinib mesylate in terms of the
development of resistance. However, our study indicates that clinical resistance to …
development of resistance. However, our study indicates that clinical resistance to …
[HTML][HTML] Sustained deep molecular responses in patients switched to nilotinib due to persistent BCR-ABL1 on imatinib: final ENESTcmr randomized trial results
… did patients randomized to continue imatinib. Per the study protocol, patients in the imatinib
arm with detectable BCR-ABL1 at 24 months were allowed to cross over to nilotinib. Here we …
arm with detectable BCR-ABL1 at 24 months were allowed to cross over to nilotinib. Here we …
Evidence that resistance to nilotinib may be due to BCR-ABL, Pgp, or Src kinase overexpression
FX Mahon, S Hayette, V Lagarde, F Belloc, B Turcq… - Cancer research, 2008 - AACR
… of imatinib-resistant or imatinib-intolerant disease. In the current study, we generated
nilotinib-… We also tested the effect of imatinib on nilotinib-resistant cell lines, showing that the …
nilotinib-… We also tested the effect of imatinib on nilotinib-resistant cell lines, showing that the …
Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study
A Ray, SW Cowan-Jacob, PW Manley… - Blood, The Journal …, 2007 - ashpublications.org
… inhibitors, which minimize the number of residual BCR-ABL + cells capable of developing
resistance and which maintain activity against imatinib mesylate-resistant BCR-ABL mutants. …
resistance and which maintain activity against imatinib mesylate-resistant BCR-ABL mutants. …
Nilotinib versus imatinib for the treatment of patients with newly diagnosed chronic phase, Philadelphia chromosome-positive, chronic myeloid leukaemia: 24-month …
HM Kantarjian, A Hochhaus, G Saglio… - The lancet …, 2011 - thelancet.com
… 400 mg twice daily vs imatinib). At 24 months… nilotinib groups than in the imatinib group (five
with nilotinib 300 mg twice daily, three with nilotinib 400 mg twice daily, and ten with imatinib)…
with nilotinib 300 mg twice daily, three with nilotinib 400 mg twice daily, and ten with imatinib)…
Early molecular response predicts outcomes in patients with chronic myeloid leukemia in chronic phase treated with frontline nilotinib or imatinib
… molecular response (EMR; BCR-ABL ≤10% on the international scale [BCR-ABL IS ] at 3
or … with nilotinib or imatinib based on 4 years of follow up in Evaluating Nilotinib Efficacy and …
or … with nilotinib or imatinib based on 4 years of follow up in Evaluating Nilotinib Efficacy and …