Overview

Generic Name(s):
entospletinib
NCI Definition [1]:
An orally available inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. Upon oral administration of entospletinib, this agent may inhibit the activity of Syk, which inhibits B-cell receptor (BCR) signaling and leads to an inhibition of tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoeitic malignancies.

Entospletinib has been investigated in 3 clinical trials, of which 1 is open and 2 are closed. Of the trials investigating entospletinib, 3 are phase 1/phase 2 (1 open).

MS4A1 Expression, NPM1 Mutation, and PML-RARA Fusion are the most frequent biomarker inclusion criteria for entospletinib clinical trials.

Acute myeloid leukemia, B-cell prolymphocytic leukemia, and chronic lymphocytic leukemia/small lymphocytic lymphoma are the most common diseases being investigated in entospletinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Entospletinib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Entospletinib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating entospletinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
gs-9973, imidazo(1,2-a)pyrazin-8-amine, 6-(1h-indazol-6-yl)-n-(4-(4-morpholinyl)phenyl)-, syk inhibitor gs-9973, 6-(1h-indazol-6-yl)-n-(4-(morpholin-4-yl)phenyl)imidazo(1,2-a)pyrazin-8-amine, ento, 1229208-44-9, gs 9973, 6-(1h-indazol-6-yl)-n-(4-(morpholin-4-yl)phenyl)imidazo(1,2-a)pyrazin-8-amine, entospletinib, spleen tyrosine kinase inhibitor gs-9973
Drug Categories [2]:
Tyrosine kinase inhibitors
Drug Target(s) [2]:
SYK
NCIT ID [1]:
C105402

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.