Drug intelligence / Profile preview

dasatinib + chemotherapy

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Intrathecal
01

Overview

Dasatinib + chemotherapy refers to the combination of **dasatinib**, a multi-kinase inhibitor primarily targeting BCR-ABL and KIT kinases, with standard cytotoxic chemotherapy regimens. This combination is not a fixed-dose combination product but rather represents a protocol in which dasatinib is added to conventional chemotherapeutic agents (such as cytarabine and daunorubicin) for the treatment of certain leukemias. Mechanistically, dasatinib inhibits kinase signaling involved in cell proliferation and survival, particularly in leukemic cells exhibiting aberrant activation of the KIT or BCR-ABL pathway. This combination has been investigated primarily in: - **Core binding factor acute myeloid leukemia (CBF AML):** where dasatinib is added to cytarabine and daunorubicin induction and high-dose cytarabine consolidation. - **Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL):** where dasatinib is combined with multi-agent chemotherapy protocols in children and young adults. Chemotherapy refers to standard regimens, such as “7+3” (cytarabine + daunorubicin) for AML or multi-agent induction for ALL[1][2][3]. This combination aims to improve remission rates, overcome resistance due to KIT mutations (CBF AML), or provide an alternative to other tyrosine kinase inhibitors (Ph+ ALL).

02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)SFK (SRC family kinases)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)DNACSF1R (Macrophage colony-stimulating factor receptor)PDGFR (PDGFR family)FLT3 (Fms related receptor tyrosine kinase 3)EPHA2 (Ephrin type-A receptor 2)

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