AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL

E Weisberg, P Manley, J Mestan… - British journal of …, 2006 - nature.com
… and development of AMN107 is discussed, as is the current status of AMN107 in clinical …
of mechanisms of resistance to AMN107, and how and where AMN107 is expected to fit into 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
AMN107 is a new higher-potency inhibitor of BCR-ABL. To identify mutations in BCR-ABL
that could result in resistance to AMN107, a cDNA library of BCR-ABL mutants was introduced …

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
… Having characterized nilotinib (AMN107) against a large panel of imatinib mesylate–resistant
Bcr-Abl mutants, we investigated which mutants might arise under nilotinib therapy using a …

Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is active in patients with imatinib-resistant or-intolerant accelerated-phase chronic …

P Le Coutre, OG Ottmann, F Giles… - Blood, The Journal …, 2008 - ashpublications.org
Nilotinib (Tasigna [nilotinib], formerly known as AMN107; … the Bcr-Abl tyrosine kinase than
imatinib. Like imatinib, it acts through competitive inhibition of the ATP binding site of BCR-ABL

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 was effective in patients harboring BCR-ABL … resistance mechanism independent
of BCR-ABL mutations. Adverse … In summary, nilotinib is highly active and safe in patients with …

Hematologic and Cytogenetic Response Dynamics to Nilotinib (AMN107) Depend on the Type of BCR-ABL Mutations in Patients with Chronic Myelogeneous …

A Hochhaus, P Erben, S Branford, J Radich, DW Kim… - Blood, 2006 - Elsevier
… , nilotinib … of nilotinib was also demonstrated in 32/33 Im-resistant mutant cell lines. We
sought to investigate the efficacy of nilotinib in vivo according to the type of preexisting BCR-ABL

The tyrosine kinase inhibitor AMN107 (Nilotinib) exhibits off-target effects in lymphoblastic cell lines

KU Chow, D Nowak, B Trepohl, S Hochmuth… - Leukemia & …, 2007 - Taylor & Francis
… Although the AMN107-sensitive cell lines DOHH-… AMN107-resistant T-cell lines. In conclusion,
this is the first report providing evidence that activity of AMN107 is not restricted to Bcr-Abl, …

[HTML][HTML] Efficacy of Nilotinib (AMN107) in Patients (Pts) with Newly Diagnosed, Previously Untreated Philadelphia Chromosome (Ph)-Positive Chronic Myelogenous …

J Cortes, S O'Brien, E Jabbour, A Ferrajoli, G Borthakur… - Blood, 2007 - Elsevier
… Methods: We evaluated the efficacy of nilotinib as first line therapy … (BCR-ABL/ABL ratio
≤0.05% in our lab) at 12 months (mo). Results: Thirty-two pts have been treated with nilotinib

Preliminary Activity of Nilotinib (AMN107), a Novel Selective Potent Oral Bcr-Abl Tyrosine Kinase Inhibitor, in Newly Diagnosed Philadelphia Chromosome (Ph) …

E Jabbour, J Cortes, F Giles, S O'Brien, L Letvak… - Blood, 2006 - Elsevier
Nilotinib is a novel, highly selective oral Bcr-Abl inhibitor which is approximately 30-fold more
potent than imatinib. High response rates with nilotinib were observed in all CML phases …

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
AMN107 (nilotinib) are potent alternate Abl inhibitors with activity against many imatinib
mesylate–resistant BCR-ABL … )–exposed Ba/F3-p210 BCR-ABL cells to compare incidence and …