Preclinical Development of Tuspetinib for the Treatment of Acute Myeloid Leukemia

Cancer Res Commun. 2025 Jan 1;5(1):74-83. doi: 10.1158/2767-9764.CRC-24-0258.

Abstract

This article reports preclinical development of TUS, an oral kinase inhibitor currently in clinical development for treatment of AML. The article covers the studies of TUS activities on cellular targets and the nonclinical studies that supported the advancement of TUS to a phase I/II trial of TUS/VEN in refractory AML and a phase I/II trial of TUS/VEN/5-azacytidine in newly diagnosed patients with AML (NCT03850574).

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Clinical Trials, Phase I as Topic
  • Drug Evaluation, Preclinical
  • Humans
  • Leukemia, Myeloid, Acute* / drug therapy
  • Mice
  • Protein Kinase Inhibitors* / pharmacology
  • Protein Kinase Inhibitors* / therapeutic use
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use

Substances

  • Protein Kinase Inhibitors
  • Pyrimidines
  • Antineoplastic Agents

Associated data

  • ClinicalTrials.gov/NCT03850574