Tas-102: A novel antimetabolite for the 21st century

Nataliya Uboha, Howard S. Hochster

Research output: Contribution to journalArticlepeer-review

20 Scopus citations

Abstract

TAS-102, a novel antimetabolite combination chemotherapy agent, consists of a rediscovered antimetabolite agent, trifluorothymidine (trifluridine) combined with the metabolic inhibitor of thymidine phosphorylase, tipiracil, in a 1:0.5 molar ratio. Mechanism of action studies suggest that this agent works by incorporation into DNA. Both preclinical and clinical studies demonstrate that this agent is noncross-resistant with 5-fluorouracil. Tipiracil may also have antiangiogenic effects through inhibition of thymidine phosphorylase. Recent randomized Phase II and III trials demonstrate clinical activity (improved progression-free survival, time to decrease in performance status, prolonged overall survival) in metastatic colorectal cancer refractory to all standard agents. Monotherapy with TAS-102 has now been approved for this indication in Japan and in the USA.

Original languageEnglish (US)
Pages (from-to)153-163
Number of pages11
JournalFuture Oncology
Volume12
Issue number2
DOIs
StatePublished - Jan 2016
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Oncology
  • Cancer Research

Keywords

  • Antiangiogenesis
  • Colorectal cancer
  • Fluoropyrimidine resistance
  • Fluoropyrimidines
  • TAS-102
  • Trifluorothymidine

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