Drug intelligence / Profile preview

dasatinib

Development stage
Approved
Lead developer
Bristol Myers Squibb
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
01

Overview

Dasatinib is an orally administered small molecule tyrosine kinase inhibitor primarily used to treat Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) in both adults and children aged 1 year or older. It works by inhibiting the activity of multiple kinases, most notably the BCR-ABL fusion protein produced by the Philadelphia chromosome abnormality. This inhibition blocks signals that promote cancer cell proliferation and survival. Dasatinib also targets several SRC-family kinases and other oncogenic kinases involved in leukemogenesis. It is effective against some forms of CML or ALL that are resistant to imatinib due to certain mutations in the ABL kinase domain[1][4][7]. The drug was originally developed by Bristol Myers Squibb.

Brand names
SprycelPhyragoDasanixNextki
Other names
BMS-354825BMS354825BMS 354825
02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)EPHA2 (Ephrin type-A receptor 2)KIT (c-KIT proto-oncogene receptor tyrosine kinase)TEC (TEC proto-oncogene tyrosine-protein kinase)BTK (Bruton tyrosine kinase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)SFK (SRC family kinases)

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