Small molecule FLT3 tyrosine kinase inhibitors

Related Experiment Video

Updated: Aug 24, 2026

Comet Assay to Quantify DNA Damage in FLT3 Mutant-expressing 32D Cells after Exposure to Type I and Type II FLT3 Inhibitors
04:36

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

Published on: October 17, 2025

Mark Levis1, Donald Small

  • 1Johns Hopkins University School of Medicine, Department of Oncology, Baltimore, Maryland, USA.

Current Pharmaceutical Design
|April 14, 2004
PubMed

Insights

Activating mutations in FMS-Like Tyrosine kinase-3 (FLT3) are common in acute myeloid leukemia (AML) and linked to poor outcomes. This review details novel FLT3 inhibitors developed to target these mutations and assesses their clinical utility.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Activating mutations in FMS-Like Tyrosine kinase-3 (FLT3) represent the most frequent molecular alteration in acute myeloid leukemia (AML).
  • FLT3 mutations are strongly correlated with a poorer prognosis in AML patients.
  • This has driven the development of targeted therapies.

Purpose of the Study:

  • To review the latest developments in small molecule FLT3 tyrosine kinase inhibitors.
  • To compare and contrast these novel agents.
  • To evaluate their clinical potential and the assays used for characterization.

Main Methods:

  • Literature review of recent studies on FLT3 inhibitors in AML.
  • Comparative analysis of different FLT3 inhibitors.
  • Assessment of preclinical and clinical data.

Main Results:

  • Several novel small molecule FLT3 inhibitors have been developed.
  • These agents show varying degrees of efficacy and specificity.
  • Characterization assays differ across studies.

Conclusions:

  • FLT3 inhibitors represent a promising therapeutic strategy for AML with FLT3 mutations.
  • Further research is needed to optimize treatment selection and overcome resistance.
  • Understanding assay methodologies is crucial for comparing drug efficacy.

More Related Videos

Experimental Melanoma Immunotherapy Model Using Tumor Vaccination with a Hematopoietic Cytokine09:15

Experimental Melanoma Immunotherapy Model Using Tumor Vaccination with a Hematopoietic Cytokine

Published on: February 24, 2023

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...