Dasatinib for the treatment of Philadelphia chromosome-positive leukemias.

Abstract

INTRODUCTION:

Dasatinib is a dual Abl/Src tyrosine kinase inhibitor (TKI), which was developed to treat patients with chronic myelogenous leukemia (CML), who had failed or were intolerant to therapy with imatinib.

AREAS COVERED:

In this article, we review preclinical and clinical studies with dasatinib for the therapy of Philadelphia (Ph)-positive leukemias.

EXPERT OPINION:

Dasatinib is very effective in the setting of CML resistance or intolerance to imatinib, particularly in patients in chronic phase (CP). Dasatinib is also effective against most BCR-ABL1 mutations that arise during therapy with imatinib. Further studies have confirmed activity of dasatinib as a single-agent, and combined with chemotherapy, for the treatment of patients with Philadelphia-positive acute lymphoblastic leukemia (Ph+-ALL). More recently, randomized trials have demonstrated that dasatinib is superior to imatinib in the initial therapy of patients with CML, and the drug was approved by the FDA for this indication in 2011.

• Authors: Fabio P S Santos, Jorge Cortes
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 13 Issue 16 Pg. 2381-95 (Nov 2012) ISSN: 1744-7666 [Electronic] England
• PMID: 22992064 (Publication Type: Journal Article, Review)

Chemical References

• Antineoplastic Agents
• Benzamides
• Piperazines
• Protein Kinase Inhibitors
• Pyrimidines
• Thiazoles
• Imatinib Mesylate
• Dasatinib

Topics

• Animals
• Antineoplastic Agents (pharmacology, therapeutic use)
• Benzamides
• Dasatinib
• Drug Resistance, Neoplasm
• Humans
• Imatinib Mesylate
• Piperazines (therapeutic use)
• Precursor Cell Lymphoblastic Leukemia-Lymphoma (drug therapy, metabolism)
• Protein Kinase Inhibitors (pharmacology, therapeutic use)
• Pyrimidines (therapeutic use)
• Thiazoles (therapeutic use)