LY3410738, a Covalent Inhibitor of Mutant IDH1/2, Is Effective in Acute Myeloid Leukemia Preclinical Models.

doi:10.1158/2643-3230.BCD-25-0379

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Article

LY3410738, a Covalent Inhibitor of Mutant IDH1/2, Is Effective in Acute Myeloid Leukemia Preclinical Models.

Blood cancer discovery - 3 Sept 2026

Brooks Nathan A, Skwarska Anna, Salama Vivian, Bender Mark H, Kays Lisa, DeWalt Robin I, Perria Bryan, Thete Deepti, Manro Jason R, Cavitt Rachel, Leon Rebecca, Gomez Sandra, Torres Raquel, Strelow John M, Milligan Paul, Newell Kate, Roth Kenneth D, Sarry Jean-Emmanuel, Chan Steven M, Lagutan Danalyn Manglicmot, Romero Richard, Antonysamy Stephen, Johnson Robert L, Gong Xueqian, Bauer Renato A, Burkholder Timothy P, Hahn Patric J, Rankovic Zoran, Boulet Serge L, DiNardo Courtney D, Konopleva Marina, Gilmour Raymond

Abstract excerpt

Acute myeloid leukemia (AML) is an aggressive blood disorder characterized by rapid growth of poorly differentiated myeloid cells. Gain-of-function mutations in isocitrate dehydrogenases (IDH) are detected in ∼20% of AML and ∼80% of secondary gliomas. Mutant IDH1/2 isoenzymes acquire neomorphic activity to produce 2-hydroxyglutarate (2-HG) oncometabolite, resulting in hypermethylated DNA and histones, altered...

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Topics

Isocitrate Dehydrogenase
Animals
Humans

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Leukemia, Myeloid, Acute

Mice

Mutation

Enzyme Inhibitors

Xenograft Model Antitumor Assays

Antineoplastic Agents

Cell Line, Tumor

Disease Models, Animal

Source

Open in PubMed

Identifiers

PMID: 42490065
DOI: 10.1158/2643-3230.BCD-25-0379

Genes

IDH1

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 20 Oct 2026.

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