Abstract
Imatinib mesylate is currently the standard therapy for chronic myeloid leukemia (CML) patients. Despite the remarkable results achieved with imatinib, the emergence of resistance to this drug has become a significant problem. Several strategies have been developed to overcome imatinib resistance, including dose escalation of the drug, combination treatments or novel targeted agents. Nilotinib is a second-generation tyrosine kinase inhibitor 30-50 fold more potent than imatinib with high affinity and selectivity on BCR/ABL, active against a wide range of mutant clones, except T315I mutation. Phase II trials of nilotinib showed high activity in imatinib-resistant or intolerant CML patients; front-line treatment of chronic phase Ph+ CML demonstrated rapid and stable cytogenetic responses and increasing molecular responses. We here review the development of nilotinib and the efficacy data in phase II and front-line trials.
Current Drug Targets
Title: Nilotinib Therapy in Chronic Myelogenous Leukemia: The Strength of High Selectivity on BCR/ABL
Volume: 10 Issue: 6
Author(s): Massimo Breccia and Giuliana Alimena
Affiliation:
Abstract: Imatinib mesylate is currently the standard therapy for chronic myeloid leukemia (CML) patients. Despite the remarkable results achieved with imatinib, the emergence of resistance to this drug has become a significant problem. Several strategies have been developed to overcome imatinib resistance, including dose escalation of the drug, combination treatments or novel targeted agents. Nilotinib is a second-generation tyrosine kinase inhibitor 30-50 fold more potent than imatinib with high affinity and selectivity on BCR/ABL, active against a wide range of mutant clones, except T315I mutation. Phase II trials of nilotinib showed high activity in imatinib-resistant or intolerant CML patients; front-line treatment of chronic phase Ph+ CML demonstrated rapid and stable cytogenetic responses and increasing molecular responses. We here review the development of nilotinib and the efficacy data in phase II and front-line trials.
Export Options
About this article
Cite this article as:
Breccia Massimo and Alimena Giuliana, Nilotinib Therapy in Chronic Myelogenous Leukemia: The Strength of High Selectivity on BCR/ABL, Current Drug Targets 2009; 10 (6) . https://dx.doi.org/10.2174/138945009788488468
DOI https://dx.doi.org/10.2174/138945009788488468 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Concurrent Methicillin-Resistant <i>Staphylococcus aureus Septicemia</i> and Thyroid Abscess in a Young Male with Dengue
Infectious Disorders - Drug Targets Pathophysiology of Post-Operative Low Cardiac Output Syndrome
Current Vascular Pharmacology Mesothelioma - Update on Management
Current Respiratory Medicine Reviews Left Atrial Appendage Closure -The WATCHMAN Device
Current Cardiology Reviews Regulation of Adrenomedullin and its Family Peptide by RAMP System – Lessons from Genetically Engineered Mice
Current Protein & Peptide Science Nontuberculous Mycobacterium Infections in Rheumatoid Arthritis Patients: The Serodiagnosis of Pulmonary Disease due to Mycobacterium avium Complex with an Enzyme Immunoassay Kit Detecting Glycopeptidolipid Core Antigen (Capilia MAC Antibody ELISA)<sup>®</sup>)
Current Rheumatology Reviews Evaluation of the Pulmonary Veins and Left Atrial Volume using Multidetector Computed Tomography in Patients Undergoing Catheter Ablation for Atrial Fibrillation
Current Cardiology Reviews Contemporary Treatment of Amyloid Heart Disease
Current Pharmaceutical Design Adverse Cardiovascular Effects of Antirheumatic Drugs: Implications for Clinical Practice and Research
Current Pharmaceutical Design Current Therapeutic Strategies and Future Perspectives for the Prevention of Arterial Thromboembolism: Focus on Atrial Fibrillation
Current Pharmaceutical Design Repurposing of Anticancer Drugs for the Treatment of Bacterial Infections
Current Topics in Medicinal Chemistry Clinical Applications of Cardiovascular Magnetic Resonance
Current Pharmaceutical Design Diagnosis of Systemic Lupus Erythematosus in an Unusual Presentation: What a Primary Care Physician Should Know
Current Rheumatology Reviews Cardiotoxicity of Molecularly Targeted Agents
Current Cardiology Reviews Lymphadenopathy as a Prodrome for Systemic Lupus Erythematous
Current Rheumatology Reviews The Medical Complications of Anorexia Nervosa and Their Treatments
Current Women`s Health Reviews Stroke and COVID-19 Pandemic: The Dilemma
Coronaviruses Biological Agents Involved in Malignant Mesothelioma: Relevance as Biomarkers or Therapeutic Targets
Current Cancer Drug Targets Chest Pain in Children
Current Pediatric Reviews Pearls from the First Gulf Cardiac Amyloidosis Summit 2021
New Emirates Medical Journal