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Currently, you can access the following clinical trials being conducted worldwide:

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Clinical trial information and results are updated daily from ClinicalTrials.gov. The latest data update was conducted on 12/02/2020.
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Clinical trial information and results are updated daily from ClinicalTrials.gov. The latest data update was conducted on 12/02/2020.
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Our Science

    • enasidenib (IDH2 Inhibitor)

    The safety and efficacy of the agents and/or uses under investigation have not been established. There is no guarantee that the agents will receive health authority approval or become commercially available in any country for the uses being investigated.

    Proposed Mechanism of Action

    Enasidenib is an oral, reversible, selective inhibitor of mutated isocitrate dehydrogenase (IDH) 2.1,2 In vitro studies suggest that the oncometabolite 2-hydroxyglutarate (2-HG), which is present at high levels in patients with IDH mutations,3-5 may drive epigenetic changes that block normal cellular differentiation, leading to a cancerous state.2,4 As demonstrated in preclinical studies, enasidenib binds and inhibits the mutant IDH2 enzyme that is responsible for the accumulation of 2-HG.2

    Enasidenib Hypothesized Mechanism of Action

    Enasidenib is a selective inhibitor of mutant IDH2 and has been hypothesized to reduce 2-HG levels which may restore DNA demethylation in acute myeloid leukemia.

    enasidenib by Disease State

    enasidenib in Acute Myeloid Leukemia

    Phase 2
    1st line with an IDH2 Mutation

    Phase 3
    Relapsed/Refractory with an IDH2 Mutation

    View Trials Investigating enasidenib in Acute Myeloid Leukemia
    View Rationale for Clinical Development

    Rationale for Clinical Development

    IDH2 mutations occur in various cancers and occur in approximately 8% to 19% of patients with AML.5-7 Preclinical data suggest that enasidenib may have clinical activity in IDH2-mutant AML through the reduction of 2-HG levels and the induction of blast differentiation.2 In vitro studies have shown that enasidenib may reduce 2-HG levels by > 90%, reverse histone and DNA hypermethylation, and induce differentiation in leukemia cell models.2 In a primary human mutant IDH2 AML xenograft model, enasidenib reduced 2-HG levels and induced dose-dependent proliferation and differentiation.2

    View Related Pathways

    Isocitrate Dehydrogenase (IDH) Mutations

    References

    1. Stein EM, et al. Blood. 2014;124 [abstract 115].
    2. Yen K, et al. Blood. 2013;122 [abstract 240].
    3. Ward PS, et al. Cancer Cell. 2010;17:225-234. PMID: 20171147
    4. Gross S, et al. J Exp Med. 2010;207:339-344. PMID: 20142433
    5. Losman JA, Kaelin WG Jr. Genes Dev. 2013;27:836-852. PMID: 23630074
    6. Green CL, et al. Blood. 2011;118:409-412. PMID: 21596855
    7. Im AP, et al. Leukemia. 2014;28:1774-1783. PMID: 24699305