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vorasidenib

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Overview

NCI Definition [1]:
An orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity. Upon administration, vorasidenib specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations. In addition, vorasidenib is able to penetrate the blood-brain barrier (BBB). IDH1 and 2, metabolic enzymes that catalyze the conversion of isocitrate into a-KG, play key roles in energy production and are mutated in a variety of cancer cell types. In addition, mutant forms of IDH1 and 2 catalyze the formation of 2HG and drive cancer growth by blocking cellular differentiation and inducing cellular proliferation.

Clinical Trials

View Clinical Trials for vorasidenib

Vorasidenib has been investigated in 2 clinical trials, of which 2 are open and 0 are closed. Of the trials investigating vorasidenib, 1 is phase 1 (1 open) and 1 is phase 3 (1 open).

IDH1 R132H, IDH1 R132C, and IDH1 R132G are the most frequent biomarker inclusion criteria for vorasidenib clinical trials.

Astrocytoma and oligodendroglioma are the most common diseases being investigated in vorasidenib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Vorasidenib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating vorasidenib 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]:
ag 881, idh1/2 mutant inhibitor ag-881, ag881, idh mutant inhibitor ag-881, ag-881, pan idh mutant inhibitor ag-881, pan-idh mutant inhibitor ag-881
Drug Target(s) [2]:
IDH1, IDH2
NCIT ID [1]:
C152914

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.