Overview

Generic Name(s):
epacadostat
NCI Definition [1]:
An orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. Epacadostat targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, INCB024360 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs.

Epacadostat has been investigated in 27 clinical trials, of which 13 are open and 14 are closed. Of the trials investigating epacadostat, 6 are phase 1 (3 open), 10 are phase 1/phase 2 (4 open), 8 are phase 2 (5 open), and 3 are phase 3 (1 open).

Deficient DNA Mismatch Repair (dMMR), ER Negative, and ER No Expression are the most frequent biomarker inclusion criteria for epacadostat clinical trials.

Malignant solid tumor, head and neck squamous cell carcinoma, and colorectal carcinoma are the most common diseases being investigated in epacadostat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Epacadostat
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Epacadostat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating epacadostat 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]:
1204669-58-8, incb024360, ido1 inhibitor incb024360, indoleamine-2,3-dioxygenase inhibitor incb024360, epacadostat, 1,2,5-oxadiazole-3-carboximidamide, 4-((2-((aminosulfonyl)amino)ethyl)amino)-n-(3-bromo-4-fluorophenyl)-n'-hydroxy-, (c(z))-, ido1 inhibitor incb024360, incb 024360
Drug Categories [2]:
Immunotherapies
Drug Target(s) [2]:
IDO1
NCIT ID [1]:
C92582

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.