Drug intelligence / Profile preview

entospletinib + vincristine

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Entospletinib + vincristine is an experimental combination therapy evaluated for hematological malignancies, notably relapsed or refractory acute lymphoblastic leukemia (ALL). **Entospletinib** is an oral, selective inhibitor of spleen tyrosine kinase (SYK), a crucial component in B-cell receptor signaling pathways. **Vincristine** is a microtubule inhibitor classified as a vinca alkaloid, disrupting mitosis in dividing cells. Combined, these agents aim to synergistically inhibit leukemia cell proliferation and survival. Preclinical studies and early-phase clinical trials suggest enhanced antileukemic efficacy by combining entospletinib with vincristine, particularly in specific genetic subtypes of leukemia such as KMT2A-rearranged ALL[1][4][6].

02

Targets

TUBB (Tubulin (alpha and beta subunits))SYK (Spleen Tyrosine Kinase)

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