4.6 Article

Olutasidenib: from bench to bedside

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BLOOD ADVANCES
卷 7, 期 16, 页码 4358-4365

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DOI: 10.1182/bloodadvances.2023009854

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The discovery of IDH1 mutations in AML and the success of molecularly targeted therapies led to the development of IDH1mut inhibitors. Olutasidenib, a novel IDH1mut inhibitor, showed promising results in treating patients with R/R IDH1mut AML, including durable remission rates and transfusion independence. This review examines the development and positioning of olutasidenib in the treatment of IDH1mut AML.
The discovery of isocitrate dehydrogenase 1 (IDH1) mutations in acute myeloid leukemia (AML) and the resounding success of molecularly targeted therapies in related myeloid malignancies swiftly prompted the development of IDH1mut inhibitors. Olutasidenib (formerly known as FT-2102) is an orally administered novel IDH1mut inhibitor that entered clinical development in 2016, proceeded briskly through the developmental process, and was granted regular approval to treat patients with R/R IDH1mut AML on 1 December 2022. Single agent olutasidenib, a potent and selective IDH1mut inhibitor, demonstrated highly durable remission rates along with meaningful outcomes, such as transfusion independence, in patients with R/R IDH1mut AML. This review will examine the preclinical and clinical development and the positioning of olutasidenib in the IDH1mut AML treatment landscape.

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