TAS-102 for the treatment of metastatic colorectal cancer

Expert Rev Anticancer Ther. 2015;15(11):1283-92. doi: 10.1586/14737140.2015.1105746. Epub 2015 Oct 28.

Abstract

The survival of patients with metastatic colorectal cancer has notably increased in the past 20 years, from 12 months to around 30 months. Nevertheless, the prognosis of patients pretreated with all available agents is poor and there is high unmet need for newer treatments. TAS-102 is an orally administered combination of the nucleoside analogue trifluridine and tipiracil hydrochloride, a thymidine phosphorylase inhibitor. In a randomized trial of 800 patients who had received at least two other treatments previously (most patients had received more than four treatments). TAS-102 demonstrated a significant prolongation of overall survival compared with placebo (median survival 7.1 vs. 5.3 months; hazard ratio 0 · 68, 95%CI: 0 · 58-0 · 81; p < 0 · 001). The toxicity was manageable, grade 3 or higher events occurred in 69% of patients in the TAS-102 group versus 52% in the placebo group, with neutropenia the most common event.

Keywords: TAS-102; fluoropyrimidines; metastatic colorectal cancer; refractory; regorafenib.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / pathology
  • Drug Combinations
  • Humans
  • Neoplasm Metastasis
  • Prognosis
  • Pyrrolidines
  • Survival Rate
  • Thymine
  • Trifluridine / adverse effects
  • Trifluridine / pharmacology
  • Trifluridine / therapeutic use*
  • Uracil / adverse effects
  • Uracil / analogs & derivatives*
  • Uracil / pharmacology
  • Uracil / therapeutic use

Substances

  • Drug Combinations
  • Pyrrolidines
  • trifluridine tipiracil drug combination
  • Uracil
  • Thymine
  • Trifluridine