An optimal dosing schedule for a novel combination antimetabolite, TAS-102, based on its intracellular metabolism and its incorporation into DNA.

@article{Emura2004AnOD,
  title={An optimal dosing schedule for a novel combination antimetabolite, TAS-102, based on its intracellular metabolism and its incorporation into DNA.},
  author={Tomohiro Emura and Fumio Nakagawa and Akio Fujioka and Hideyuki Ohshimo and Tatsushi Yokogawa and Hiroyuki Okabe and Kenji Kitazato},
  journal={International journal of molecular medicine},
  year={2004},
  volume={13 2},
  pages={249-55}
}
TAS-102 is a combination drug consisting of alpha,alpha,alpha-trifluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). FTD is converted to F3TMP by thymidine kinase and inhibits the thymidylate synthetase (TS) activity by binding to TS. In addition, FTD triphosphate form, F3TTP is incorporated into DNA, which leads to cytocidal effects. Therefore, the incorporation of FTD into DNA is expected to be an important factor, discriminating it from 5-FU showing TS inhibitory activity as… CONTINUE READING
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