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.
Penn State Milton S. Hershey Medical Center and Children's Hospital, Hershey, Pennsylvania, United States
St. Lukes, Boise, Idaho, United States
Connecticut Children's Hospital, Hartford, Connecticut, United States
Institute of Hematology & Blood Diseases Hospital, Tianjin, Tianjin, China
Memorial Sloan Kettering Cancer Center, New York, New York, United States
Alaska Women's Cancer Care, Anchorage, Alaska, United States
Anchorage Oncology Centre, Anchorage, Alaska, United States
Katmai Oncology Group, Anchorage, Alaska, United States
Massachusetts General Hospital, Boston, Massachusetts, United States
Dana Farber Cancer Institute, Boston, Massachusetts, United States
M D Anderson Cancer Center, Houston, Texas, United States
M D Anderson Cancer Center, Houston, Texas, United States
Local Institution, Wuhan, Hubei, China
Policlinico Universitario di Milano, Milano, Italy
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