Heterogeneous resistance to quizartinib in acute myeloid leukemia revealed by single-cell analysis

Blood. 2017 Jul 6;130(1):48-58. doi: 10.1182/blood-2016-04-711820. Epub 2017 May 10.

Abstract

Genomic studies have revealed significant branching heterogeneity in cancer. Studies of resistance to tyrosine kinase inhibitor therapy have not fully reflected this heterogeneity because resistance in individual patients has been ascribed to largely mutually exclusive on-target or off-target mechanisms in which tumors either retain dependency on the target oncogene or subvert it through a parallel pathway. Using targeted sequencing from single cells and colonies from patient samples, we demonstrate tremendous clonal diversity in the majority of acute myeloid leukemia (AML) patients with activating FLT3 internal tandem duplication mutations at the time of acquired resistance to the FLT3 inhibitor quizartinib. These findings establish that clinical resistance to quizartinib is highly complex and reflects the underlying clonal heterogeneity of AML.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Research Support, Non-U.S. Gov't
  • Research Support, N.I.H., Extramural

MeSH terms

  • Benzothiazoles / administration & dosage*
  • Drug Resistance, Neoplasm* / drug effects
  • Drug Resistance, Neoplasm* / genetics
  • Female
  • High-Throughput Nucleotide Sequencing*
  • Humans
  • INDEL Mutation*
  • Leukemia, Myeloid, Acute* / drug therapy
  • Leukemia, Myeloid, Acute* / genetics
  • Male
  • Phenylurea Compounds / administration & dosage*
  • fms-Like Tyrosine Kinase 3 / genetics*

Substances

  • Benzothiazoles
  • Phenylurea Compounds
  • quizartinib
  • FLT3 protein, human
  • fms-Like Tyrosine Kinase 3