Drug intelligence / Profile preview

entospletinib + vincristine + dexamethasone

Development stage
Unknown
Lead developer
Gilead Sciences
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral (entospletinib, Dexamethasone), Intravenous (vincristine)
01

Overview

A combination therapy comprising **entospletinib** (an oral, selective spleen tyrosine kinase [SYK] inhibitor), **vincristine** (a vinca alkaloid anti-mitotic chemotherapy), and **dexamethasone** (a synthetic glucocorticoid corticosteroid), primarily studied in preclinical and early clinical settings for hematologic malignancies such as acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL). Entospletinib inhibits SYK, disrupting B-cell receptor and other signaling pathways, contributing to anti-leukemic effects, while vincristine disrupts microtubule formation, leading to cell cycle arrest, and dexamethasone exerts anti-inflammatory and lympholytic effects. Combining entospletinib with vincristine and/or dexamethasone aims to exploit potential synergistic effects against malignant hematopoietic progenitor cells, especially in AML and some lymphoid neoplasms[2][3].

02

Targets

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

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