The development of imatinib as a therapeutic agent for chronic myeloid leukemia

M Deininger, E Buchdunger, BJ Druker - Blood, 2005 - ashpublications.org
Imatinib has revolutionized drug therapy of chronic myeloid leukemia (CML). Preclinical
studies were promising but the results of clinical trials by far exceeded expectations …

Novel targeted therapies to overcome imatinib mesylate resistance in chronic myeloid leukemia (CML)

C Walz, M Sattler - Critical reviews in oncology/hematology, 2006 - Elsevier
Imatinib mesylate (Gleevec) was developed as the first molecularly targeted therapy that
specifically inhibits the BCR–ABL tyrosine kinase activity in patients with Philadelphia …

BAY 43-9006 inhibition of oncogenic RET mutants

F Carlomagno, S Anaganti, T Guida… - Journal of the …, 2006 - academic.oup.com
Background: Medullary and papillary thyroid carcinomas are often associated with
oncogenic activation of the RET tyrosine kinase. We evaluated whether the biaryl urea BAY …

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases

TA Carter, LM Wodicka, NP Shah… - Proceedings of the …, 2005 - National Acad Sciences
To realize the full potential of targeted protein kinase inhibitors for the treatment of cancer, it
is important to address the emergence of drug resistance in treated patients. Mutant forms of …

Dynamic modeling of imatinib-treated chronic myeloid leukemia: functional insights and clinical implications

I Roeder, M Horn, I Glauche, A Hochhaus… - Nature medicine, 2006 - nature.com
Abstract Treatment of chronic myeloid leukemia (CML) with the tyrosine kinase inhibitor
imatinib represents a successful application of molecularly targeted cancer therapy. A rapid …

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) …

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
Targeting the tyrosine kinase activity of Bcr-Abl is an attractive therapeutic strategy in chronic
myeloid leukemia (CML) and in Bcr-Abl–positive acute lymphoblastic leukemia. Whereas …

Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL+ progenitors via JAK-2 …

Y Wang, D Cai, C Brendel, C Barett, P Erben… - Blood, 2007 - ashpublications.org
Overcoming imatinib mesylate (IM) resistance and disease persistence in patients with
chronic myeloid leukemia (CML) is of considerable importance to the issue of potential cure …

Overexpression of the heat-shock protein 70 is associated to imatinib resistance in chronic myeloid leukemia

M Pocaly, V Lagarde, G Etienne, JA Ribeil, S Claverol… - Leukemia, 2007 - nature.com
Imatinib is an effective therapy for chronic myeloid leukemia (CML), a myeloproliferative
disorder characterized by the expression of the recombinant oncoprotein Bcr-Abl. In this …

[PDF][PDF] AMN107: tightening the grip of imatinib

T O'Hare, DK Walters, MWN Deininger, BJ Druker - Cancer cell, 2005 - cell.com
The Abl inhibitor imatinib is a highly effective therapy for patients with chronic myeloid
leukemia. Relapses are relatively uncommon in newly diagnosed patients, but are the rule …