Overcoming Resistance to FLT3-ITD Therapeutics

FLT3-ITD (internal tandem duplication) is a key driver of acute myeloid leukemia (AML), and several FDA-approved drugs target this mutant kinase. This Viewpoint describes the discovery of inhibitors targeting point mutants and the development of SILA123, a highly potent and selective type II FLT3 inhibitor. In <i>in vivo</i> studies, SILA-123 significantly suppressed tumor growth in allograft models, demonstrating its potential in treating resistant AML.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2024-12-12
DOI
https://doi.org/10.1021/acs.jmedchem.4c02878
Citations
3
Primary Topic
Acute Myeloid Leukemia Research
Type
article
Field-Weighted Citation Impact
1.36
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article

Overcoming Resistance to FLT3-ITD Therapeutics

Campbell McInnes
3 citations
Journal of Medicinal Chemistry
Acute Myeloid Leukemia Research
1.36
article

Overcoming Resistance to FLT3-ITD Therapeutics

Campbell McInnes
article en
3 citations

Abstract

FLT3-ITD (internal tandem duplication) is a key driver of acute myeloid leukemia (AML), and several FDA-approved drugs target this mutant kinase. This Viewpoint describes the discovery of inhibitors targeting point mutants and the development of SILA123, a highly potent and selective type II FLT3 inhibitor. In <i>in vivo</i> studies, SILA-123 significantly suppressed tumor growth in allograft models, demonstrating its potential in treating resistant AML.

Journal of Medicinal ChemistryVol. 67(24)
University of South Carolina Sumter (US)
Zero hunger
Openalex Percentile: Top 16%
Acute Myeloid Leukemia Research
1.36
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Overcoming Resistance to FLT3-ITD Therapeutics — Campbell McInnes · Journal of Medicinal Chemistry (2024) | TGRS Research Map | TGRS