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entospletinib + chemotherapy
- Development stage
- Unknown
- Lead developer
- Gilead Sciences
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral (entospletinib), Intravenous (chemotherapeutic Agents Such As Cytarabine, Daunorubicin, Vincristine)
01
Overview
Entospletinib + chemotherapy refers to the combination of entospletinib, a selective and potent small-molecule inhibitor of spleen tyrosine kinase (SYK), with standard chemotherapeutic agents. Entospletinib disrupts SYK-mediated signal transduction, which is critical in the pathogenesis of several hematologic malignancies. The combination is being studied primarily for the treatment of **acute myeloid leukemia (AML)**, including specific genetic subgroups such as *NPM1*-mutated AML and KMT2A-rearranged (MLL-r) leukemias, as well as pediatric acute lymphoblastic leukemia (ALL). Preclinical and early clinical studies suggest entospletinib enhances the antileukemic effects of chemotherapy, particularly in genetically defined subgroups like HOXA9/MEIS1 overexpression. The combination is typically administered with chemotherapies such as cytarabine and daunorubicin (the "7+3" induction regimen) or vincristine in research settings[1][3][5].
- Other names
- entospletinib plus chemotherapy
02
Targets
SYK (Spleen Tyrosine Kinase)
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