Drugs /

crenigacestat

Back to Drugs List

Overview

NCI Definition [1]:
An orally available inhibitor of the integral membrane protein gamma-secretase (GS), with potential antineoplastic activity. Upon administration, crenigacestat binds to the GS protease complex, thereby blocking the proteolytic cleavage and release of the Notch intracellular domain (NICD), which would normally follow ligand binding to the extracellular domain of the Notch receptor. This prevents both the subsequent translocation of NICD to the nucleus to form a transcription factor complex and the expression of Notch-regulated genes. This results in the induction of apoptosis and the inhibition of growth in tumor cells that overexpress Notch. Overexpression of the Notch signaling pathway plays an important role in tumor cell proliferation and survival.

Clinical Trials

View Clinical Trials for crenigacestat

Crenigacestat has been investigated in 5 clinical trials, of which 2 are open and 3 are closed. Of the trials investigating crenigacestat, 4 are phase 1 (1 open) and 1 is phase 1/phase 2 (1 open).

ER Negative, ER No Expression, and HER2 Deficient Expression are the most frequent biomarker inclusion criteria for crenigacestat clinical trials.

Multiple myeloma, breast carcinoma, and cholangiocarcinoma are the most common diseases being investigated in crenigacestat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Crenigacestat
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Crenigacestat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating crenigacestat 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]:
jsmd194, bms-986405, ly-3039478, ly 3039478, 1421438-81-4, gamma-secretase inhibitor ly3039478, ly3039478, 4,4,4-trifluoro-n-((s)-1-(((s)-5-(2-hydroxyethyl)-6-oxo-6,7-dihydro-5h-benzo[d]pyrido[2,3-b]azepin-7-yl)amino)-1-oxopropan-2-yl)butanamide
Drug Target(s) [2]:
NOTCH1, NOTCH2, NOTCH3, NOTCH4
NCIT ID [1]:
C171871

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.