Yazarlar : Breccia M, Alimena G.

Yayın : BioDrugs

Yayın Yılı : 2011

Pubmed Linki : http://www.ncbi.nlm.nih.gov/pubmed/21528941

Konu : Lösemi

Literatür İçeriği :  

Abstract

Dasatinib is an oral dual tyrosine kinase inhibitor active against ABL1 and SRC family kinases. The US FDA approved it for the treatment of chronic myeloid leukemia (CML) patients in chronic, accelerated, or blastic phase with resistance or intolerance to imatinib therapy. Dasatinib is also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia who have become resistant to or intolerant of other treatments. The agent is now also approved for newly diagnosed chronic phase (CP) patients. This article reviews the pharmacokinetic and pharmacodynamic properties of dasatinib as well as clinical data limited to CP-CML patients. Four-year follow-up of a phase III dose-optimization trial confirmed that better progression-free survival (66%) and overall survival (82%) were obtained with a dose of 100 mg once daily (od) than with the standard 70 mg twice daily dosing (65% and 75%, respectively). The 100 mg od dosing schedule was also associated with the highest benefit-risk ratio for CP patients with resistant, intolerant, or suboptimal response. Recent results of a phase III trial in newly diagnosed patients demonstrated that dasatinib 100 mg od has superiority in terms of confirmed cytogenetic and molecular responses, with faster responses and high activity in high Sokal risk patients compared with standard-dose imatinib.

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