Evaluation of the L-stereoisomeric nucleoside analog troxacitabine for the treatment of acute myeloid leukemia

Alfonso Quintás-Cardama, Jorge Cortes

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

Troxacitabine (BCH-4556; [-]-2′-deoxy-3′-oxacytidine) is a synthetic dioxolane that represents the first nucleoside analog with an L-isomer configuration to have shown important cytotoxic activity. Troxacitabine was obtained by exchanging the sulfur endocyclic atom with oxygen in the structure of lamivudine (3TC). Its unnatural stereochemistry renders it insensitive to some mechanisms of resistance of tumor cells to D-nucleosides, such as deamination by deoxycytidine deaminase and decreased active uptake by nucleoside transporters. These characteristics make troxacitabine a suitable alternative for patients with acute myelogenous leukemia as a potential way for overcoming resistance to ara-C therapy, which is the mainstay of acute myelogenous leukemia therapy at present. Clinically significant activity has been reported in Phase I studies in patients with advanced hematologic malignancies and has prompted troxacitabine to enter a series of Phase II trials in patients with refractory and relapsed acute myelogenous leukemia.

Original languageEnglish (US)
Pages (from-to)547-557
Number of pages11
JournalExpert Opinion on Investigational Drugs
Volume16
Issue number4
DOIs
StatePublished - Apr 1 2007
Externally publishedYes

Keywords

  • Leukemia
  • Nucleoside analogs
  • Troxacitabine

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Fingerprint Dive into the research topics of 'Evaluation of the L-stereoisomeric nucleoside analog troxacitabine for the treatment of acute myeloid leukemia'. Together they form a unique fingerprint.

  • Cite this