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umbralisib

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Overview

NCI Definition [1]:
An orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K) with potential antineoplastic activity. PI3K-delta inhibitor TGR-1202 inhibits PI3K and prevents the activation of the PI3K/AKT kinase signaling pathway. This decreases proliferation and induces cell death in susceptible tumor cells. Unlike other isoforms of PI3K, PI3K-delta is expressed primarily in tumor cells and cells of the hematopoietic lineage. The targeted inhibition of PI3K-delta allows for PI3K signaling in normal, non-neoplastic cells. PI3K, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival.

Clinical Trials

View Clinical Trials for umbralisib

Umbralisib has been investigated in 21 clinical trials, of which 19 are open and 2 are closed. Of the trials investigating umbralisib, 3 are phase 1 (3 open), 4 are phase 1/phase 2 (3 open), 12 are phase 2 (11 open), and 2 are phase 2/phase 3 (2 open).

CCND1 Overexpression, IGH-CCND1 Fusion, and MS4A1 Expression are the most frequent biomarker inclusion criteria for umbralisib clinical trials.

Chronic lymphocytic leukemia, follicular lymphoma, and mantle cell lymphoma are the most common diseases being investigated in umbralisib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Umbralisib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Umbralisib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating umbralisib 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]:
rp-5264, 2-((1s)-1-(4-amino-3-(3-fluoro-4-(1-methylethoxy)phenyl)-1h-pyrazolo(3,4-d)pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4h-1-benzopyran-4-one, tgr-1202, rp5264
Drug Target(s) [2]:
PIK3CD
NCIT ID [1]:
C104413

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.