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Comet Assay to Quantify DNA Damage in FLT3 Mutant-expressing 32D Cells after Exposure to Type I and Type II FLT3 Inhibitors
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Comet Assay to Quantify DNA Damage in FLT3 Mutant-expressing 32D Cells after Exposure to Type I and Type II FLT3 Inhibitors

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Lestaurtinib: a multi-targeted FLT3 inhibitor

Amir T Fathi1, Mark Levis

  • 1Department of Oncology, Division of Hematologic Malignancies, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, 1650 Orleans Street, Baltimore, MD 21231, USA.

Expert Review of Hematology
|November 19, 2010
PubMed

Insights

Internal tandem duplications in FMS-like tyrosine kinase-3 (FLT3) impact acute myelogenous leukemia outcomes. Lestaurtinib, an FLT3 inhibitor, is being investigated in ongoing clinical trials for leukemia treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Internal tandem duplications (ITDs) in FMS-like tyrosine kinase-3 (FLT3) are linked to poor prognosis in acute myelogenous leukemia (AML).
  • Targeting FLT3 is a key strategy for improving outcomes in AML patients with FLT3 mutations.

Purpose of the Study:

  • To summarize the pharmacological development of lestaurtinib, a potent FLT3 inhibitor.
  • To review the preclinical and clinical investigations of lestaurtinib in leukemia.

Main Methods:

  • Review of historical development and pharmacological properties of lestaurtinib.
  • Summary of preclinical data and ongoing clinical trial findings for lestaurtinib in AML.

Main Results:

  • Lestaurtinib is a multi-targeted indolocarbazole derivative with potent in vitro FLT3 autophosphorylation inhibition.
  • Lestaurtinib has been extensively studied in clinical trials, with multiple late-phase trials ongoing.

Conclusions:

  • Lestaurtinib represents a significant therapeutic candidate for AML patients with FLT3 mutations.
  • Ongoing clinical studies will further define the role and efficacy of lestaurtinib in treating adult and pediatric leukemia.

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