FMS-like tyrosine kinase 3 inhibitors: a patent review

Expert Opin Ther Pat. 2011 Apr;21(4):483-503. doi: 10.1517/13543776.2011.560115. Epub 2011 Feb 17.

Abstract

Introduction: Flt3 (FMS-like tyrosine kinase 3) has been presented as a target for novel anti-leukemic drugs because Flt3 mutations have been observed in acute myeloid leukemia (AML) cells. Due to both the poor efficacy and high toxicity of current standard AML therapies, there is an unmet need for new, improved therapies. Flt3 inhibitors have great potential to address this with mutated Flt3.

Areas covered: This paper provides a comprehensive review of the Flt3 inhibitor patents currently available. Information from original research articles in peer-reviewed journals and current clinical developments from several resources is also described.

Expert opinion: Our understanding of Flt3 inhibitors has been increased by findings from recent preclinical and clinical trials. Some Flt3 inhibitors show good efficacy in AML patients, but relapse and resistance to these inhibitors are still unavoidable. To address these problems, structurally diverse inhibitors, which exhibit inhibitory activities against both wild type and mutated Flt3, should be explored.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Indoles / pharmacology
  • Patents as Topic*
  • Polycyclic Compounds / pharmacology
  • Protein Kinase Inhibitors / pharmacology*
  • Quinazolines / pharmacology
  • Thiophenes / pharmacology
  • fms-Like Tyrosine Kinase 3 / antagonists & inhibitors*

Substances

  • Indoles
  • Polycyclic Compounds
  • Protein Kinase Inhibitors
  • Quinazolines
  • Thiophenes
  • fms-Like Tyrosine Kinase 3