Drug Design, Development and Therapy
Open access peer-reviewed scientific and medical journals.
Dove Medical Press is now a member of the Open Access Initiative
An Author's Guide
A guide to help authors get their paper published.
Support Open Access and Dove Press
Promotional Article Monitoring - further details
Favored Author Program
Real benefits for authors, including fast-track processing of papers.
Development and targeted use of nilotinib in chronic myeloid leukemia
(7451) Total Article Views
Authors: Carmen Fava, Hagop Kantarjian, Jorge Cortes, Elias Jabbour
Published Date November 2008
Volume 2008:2 Pages 233 - 243
Carmen Fava, Hagop Kantarjian, Jorge Cortes, Elias Jabbour
Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, Texas, USA
Abstract: The development of imatinib has resulted in sustained hematologic and cytogenetic remissions in all phases of chronic myeloid leukemia (CML). Despite the high efficacy, relapses have been observed and are much more prevalent in patients with advanced disease. The most common mechanism of acquired resistance has been traced to Bcr-Abl kinase domain mutations. Several strategies have been developed to overcome the problem of imatinib resistance, including imatinib dose escalation, novel targeted agents and combination treatments. A second generation of tyrosine kinase inhibitors was developed, which displays increased potency towards Bcr-Abl and is able to target the majority of CML mutant clones. Nilotinib (Tasigna®, AMN107, Novartis) is a close analog of imatinib with approximately 20-fold higher potency for BCR-ABL kinase inhibition. Preclinical and clinical investigations demonstrate that nilotinib effectively overcomes imatinib resistance, and has induced high rates of hematologic and cytogenetic responses in CML post imatinib failure, with a good tolerance. Nilotinib has been approved for CML patients in chronic and accelerated phases, post imatinib failure.
Keywords: nilotinib, imatinib-resistance, imatinib-intolerance, CML
Cannotea Citeulike Del.icio.us Facebook LinkedIn Twitter
Other articles by Dr Elias Jabbour
Readers of this article also read:
"I was impressed at the rapidity of publication from submission to final acceptance." Dr Edwin Thrower, PhD, Yale University.
- The benefits and risks of testosterone replacement therapy: a review
- Enzalutamide: an evidence-based review of its use in the treatment of prostate cancer
- Tumor necrosis factor-alpha inhibitor treatment for sarcoidosis
- Tenofovir-associated bone density loss