Drug intelligence / Profile preview

entospletinib

Development stage
Phase 3
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Entospletinib is a selective, orally available small molecule inhibitor of spleen tyrosine kinase (SYK), an enzyme involved in B-cell receptor signaling. By inhibiting SYK, entospletinib blocks B cell receptor-mediated signaling and proliferation in B lymphocytes. This mechanism disrupts tumor cell activation, migration, adhesion, and proliferation—processes implicated in the pathogenesis of various B-cell malignancies such as chronic lymphocytic leukemia (CLL), follicular lymphoma, mantle cell lymphoma, and other non-Hodgkin lymphomas. Entospletinib is being developed primarily for oncology indications and has also been evaluated for autoimmune diseases. The drug was developed by Gilead Sciences[1][3][4][5].

Other names
1229208-44-96-(1H-Indazol-6-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazin-8-amineentospletinib [INN]
02

Targets

ABCG2 (Breast cancer resistance protein)SYK (Spleen Tyrosine Kinase)

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