The expanding role of nilotinib in chronic myeloid leukemia
| Autor: | Theo D. Kim, Philipp le Coutre |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Oncology
medicine.medical_specialty Drug-Related Side Effects and Adverse Reactions medicine.drug_class Antineoplastic Agents medicine.disease_cause Philadelphia chromosome Piperazines Tyrosine-kinase inhibitor Leukemia Myelogenous Chronic BCR-ABL Positive hemic and lymphatic diseases Internal medicine Humans Medicine Pharmacology (medical) Protein Kinase Inhibitors Mutation business.industry Myeloid leukemia Imatinib General Medicine Protein-Tyrosine Kinases medicine.disease Pyrimidines Protein kinase domain Nilotinib Drug Resistance Neoplasm Benzamides Imatinib Mesylate business Tyrosine kinase medicine.drug |
| Zdroj: | Expert Opinion on Drug Safety. 10:97-107 |
| ISSN: | 1744-764X 1474-0338 |
| Popis: | Several therapeutic options, including tyrosine kinase inhibitors, exist for the treatment of patients with Philadelphia chromosome (Ph)-positive chronic myeloid leukemia (CML). Despite impressive results, there is room for improvement for those patients who are either resistant or intolerant to imatinib.An overview is given on the clinical results with nilotinib, a rationally designed second-generation tyrosine kinase inhibitor, as first- and second-line therapy in patients with Ph-positive CML. Important factors in predicting resistance to nilotinib and guiding therapeutic decisions are addressed.Knowledge on the clinical efficacy and safety of nilotinib after imatinib failure and as first-line treatment. Point mutations in the kinase domain (KD) of BCR-ABL1 are important determinants of clinical sensitivity to currently available tyrosine kinase inhibitors, including nilotinib. Information on specific BCR-ABL1 KD mutations and safety profiles assist in therapeutic decision making.Nilotinib is a highly effective and well-tolerated therapeutic option in patients with Ph-positive CML after imatinib failure. Early evidence demonstrating increased efficacy has allowed expanding nilotinib to previously untreated patients in chronic phase. Insights into mechanisms of resistance to tyrosine kinase inhibitors and predictive factors for response will allow for a more individualized use of these agents. |
| Databáze: | OpenAIRE |
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