ArticleCancer research2014
FLT3 kinase inhibitor TTT-3002 overcomes both activating and drug resistance mutations in FLT3 in acute myeloid leukemia.
Article in Cancer research, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 26 citations in OpenAlex.
- Molecular profile of FLT3-mutated relapsed/refractory patients with AML in the phase 3 ADMIRAL study of gilteritinib.Blood advances · 2022Trial
- XY0206 targets FLT3-dependent resistance states in acute myeloid leukemia.The Journal of clinical investigation · 2026Article
- Directed discovery of high-loading nanoaggregates enabled by drug-matched oligo-peptide excipients.Chem · 2025Article
- Functional and Structural Characterization of Clinical-Stage Janus Kinase 2 Inhibitors Identifies Determinants for Drug Selectivity.Journal of medicinal chemistry · 2024Article
- Developments of Fms-like Tyrosine Kinase 3 Inhibitors as Anticancer Agents for AML Treatment.Current medicinal chemistry · 2024Review
- Update on Small Molecule Targeted Therapies for Acute Myeloid Leukemia.Current treatment options in oncology · 2023Review
- A review of FLT3 inhibitors in acute myeloid leukemia.Blood reviews · 2022Review
- A method for overcoming plasma protein inhibition of tyrosine kinase inhibitors.Blood cancer discovery · 2021Article
- Potential targeting of FLT3 acute myeloid leukemia.Haematologica · 2021Review
- Review
- FLT3 inhibitors in acute myeloid leukemia.Journal of hematology & oncology · 2018Review
- Heat shock protein 90 inhibitors overcome the resistance to Fms-like tyrosine kinase 3 inhibitors in acute myeloid leukemia.Oncotarget · 2018Article
- Mechanisms of Resistance to FLT3 Inhibitors and the Role of the Bone Marrow Microenvironment.Hematology/oncology clinics of North America · 2017Review
- FLT3 activating mutations display differential sensitivity to multiple tyrosine kinase inhibitors.Oncotarget · 2017Article
- Identification of an orally available compound with potent and broad FLT3 inhibition activity.Oncogene · 2016Article
- Targeting BTK for the treatment of FLT3-ITD mutated acute myeloid leukemia.Scientific reports · 2015Article
- Targeted Therapy of FLT3 in Treatment of AML-Current Status and Future Directions.Journal of clinical medicine · 2014Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
There have been a number of clinical trials testing the efficacy of FMS-like tyrosine kinase-3 (FLT3) tyrosine kinase inhibitors (TKI) in patients with acute myeloid leukemia (AML) harboring a constitutively activating mutation in FLT3. However, there has been limited efficacy, most often because of inadequate achievement of FLT3 inhibition through a variety of mechanisms. In a previous study, TTT-3002 was identified as a novel FLT3 inhibitor with the most potent activity to date against FLT3 internal tandem duplication (FLT3/ITD) mutations. Here, the activity of TTT-3002 is demonstrated against a broad spectrum of FLT3-activating point mutations, including the most frequently occurring D835 mutations. The compound is also active against a number of point mutations selected for in FLT3/ITD alleles that confer resistance to other TKIs, including the F691L gatekeeper mutation. TTT-3002 maintains activity against patients with relapsed AML samples that are resistant to sorafenib and AC220. Studies utilizing human plasma samples from healthy donors and patients with AML indicate that TTT-3002 is only moderately protein bound compared with several other TKIs currently in clinical trials. Tumor burden of mice in a FLT3 TKI-resistant transplant model is significantly improved by oral dosing of TTT-3002. Therefore, TTT-3002 has demonstrated preclinical potential as a promising new FLT3 TKI that may overcome some of the limitations of other TKIs in the treatment of FLT3-mutant AML. Cancer Res; 74(18); 5206-17. ©2014 AACR.
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