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 language | English (US) |
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Pages (from-to) | 153-163 |
Number of pages | 11 |
Journal | Future Oncology |
Volume | 12 |
Issue number | 2 |
DOIs | |
State | Published - Jan 2016 |
Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Oncology
- Cancer Research
Keywords
- Antiangiogenesis
- Colorectal cancer
- Fluoropyrimidine resistance
- Fluoropyrimidines
- TAS-102
- Trifluorothymidine