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, or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

History of changes in EMA indication

  • 2016-04-25: Initial authorization

History of changes in Health Canada indication

  • 2018-01-25: Initial notice of compliance

History of changes in PMDA indication

  • 2014-03-24: Initial approval for the treatment of unresectable advanced or recurrent colorectal cancer (for use only if refractory or intolerant to standard therapies).
  • 2015-03-20: Revised indication for the treatment of unresectable advanced or recurrent colorectal cancer.
  • 2019-08-22: New indication for the treatment of unresectable advanced or recurrent gastric cancer that have progressed after chemotherapy.

Also known as

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

References