Trifluridine and tipiracil (Lonsurf)

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General information

Class/mechanism: Combination of a thymidine-based (pyrimidine) nucleoside analog, trifluridine, and a thymidine phosphorylase inhibitor, tipiracil, at a molar ratio 1:0.5 (weight ratio 1:0.471). Tipriacil inhibits the metabolism of trifluridine by thymidine phosphorylase, which increases the exposure of cancer cells to trifluridine. The thymidine-based nucleoside analog trifluridine is incorporated into DNA and disrupts DNA synthesis and cell proliferation.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Also known as

  • Code name: TAS-102
  • Generic names: trifluridine/tipiracil, trifluridine & tipiracil
  • Brand name: Lonsurf

References

  1. 1.0 1.1 1.2 Trifluridine and tipiracil (Lonsurf) package insert
  2. Trifluridine and tipiracil (Lonsurf) package insert (locally hosted backup)
  3. Lonsurf manufacturer's website