Overview

Trade Name(s):
Idhifa
NCI Definition [1]:
An orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. Upon administration, enasidenib specifically inhibits various mutant forms of IDH2, including the IDH2 variants R140Q, R172S, and R172K, which inhibits the formation of 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH2-expressing tumor cells. IDH2, an enzyme in the citric acid cycle, is mutated in a variety of cancers; it initiates and drives cancer growth by blocking differentiation and the production of the oncometabolite 2HG.

Biomarker-Directed Therapies

Enasidenib has been investigated in 15 clinical trials, of which 14 are open and 1 is closed. Of the trials investigating enasidenib, 6 are phase 1 (6 open), 3 are phase 1/phase 2 (3 open), and 6 are phase 2 (5 open).

IDH2 Mutation, PML-RARA Fusion, and t(15;17)(q22;q12) are the most frequent biomarker inclusion criteria for enasidenib clinical trials.

Acute myeloid leukemia, myelodysplastic syndromes, and chronic myelomonocytic leukemia are the most common diseases being investigated in enasidenib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Enasidenib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Enasidenib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating enasidenib 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]:
Idhifa
Drug Target(s) [2]:
IDH2

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.