Dasatinib is an orally available multikinase inhibitor indicated for the treatment of Philadelphia chromosome (Ph)-positive leukemias. Ph is a chromosomal abnormality found in patients with chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL), where the ABL tyrosine kinase and the breakpoint cluster region (BCR) gene transcribe the chimeric protein BCR-ABL. BCR-ABL is associated with the uncontrolled activity of the ABL tyrosine kinase and is involved in the pathogenesis of CML and 15-30% of ALL cases. Dasatinib also inhibits a spectrum of kinases involved in cancer, including several SRC-family kinases.
Unlike imatinib, another tyrosine kinase used for the treatment of CML and Ph-positive ALL, dasatinib inhibits the active and inactive conformations of the ABL kinase domain. Also, mutations in the kinase domain of BCR-ABL may lead to relapse during imatinib treatment. Since dasatinib does not interact with some of the residues involved in those mutations, the use of this drug represents a therapeutic alternative for patients with cancers that have developed imatinib-resistance. The use of dasatinib was first approved by the FDA in 2006.
Dasatinib is indicated for the treatment of newly diagnosed adults with Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase, as well as adults with chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib, and adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy. Dasatinib is also indicated for the treatment of pediatric patients 1 year of age and older with Ph+ CML in chronic phase or newly diagnosed Ph+ ALL in combination with chemotherapy.
University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania, United States
University of Virginia, Charlottesville, Virginia, United States
Duke University, Durham, North Carolina, United States
University of Texas MD Anderson Cancer Center, Houston, Texas, United States
University Hospital Regensburg, Department of Pediatric Hematology and Oncology, Regensburg, Germany
Freeman Hospital, Newcastle-upon-Tyne, United Kingdom
University Of Arkansas For Medical Sciences, Little Rock, Arkansas, United States
Miller Children's and Women Hospital, Long Beach, California, United States
Mountain States Tumor Institute, Boise, Idaho, United States
National Institutes of Health Clinical Center, Bethesda, Maryland, United States
OHSU Knight Cancer Institute, Portland, Oregon, United States
M D Anderson Cancer Center, Houston, Texas, United States
University of Colorado Cancer Center - Anschutz Cancer Pavilion, Aurora, Colorado, United States
University of Colorado, Denver, Colorado, United States
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