Trifluridine and tipiracil (Lonsurf)

==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.Trifluridine and tipiracil (Lonsurf) package insert Trifluridine and tipiracil (Lonsurf) package insert (locally hosted backup)Lonsurf manufacturer's website
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.
==Diseases for which it is used==
*Colorectal cancer
*Gastric cancer
==Patient drug information==
*Trifluridine and tipiracil (Lonsurf) package insert
==History of changes in FDA indication==
*2015-09-22: Approved for the treatment of patients with metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. (Based on RECOURSE)
*2019-02-22: Approved for adult patients with metastatic gastric or gastroesophageal junction (GEJ) adenocarcinoma previously treated with at least two prior lines of chemotherapy that included a fluoropyrimidine, a platinum, either a taxane or irinotecan, and if appropriate, HER2/neu-targeted therapy. (New disease entity; based on TAGS)
*2023-08-02: Approved in combination with bevacizumab, for metastatic colorectal cancer (mCRC) previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF biological therapy, and if RAS wild-type, an anti-EGFR therapy. (Based on SUNLIGHT)
==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==
Category:Drugs
Category:Combination drugs
Category:Oral medications
Category:Human DNA synthesis inhibitors
Category:Fluoropyrimidines
Category:Colorectal cancer medications
Category:Gastric cancer medications
Category:FDA approved in 2015
Category:EMA approved in 2016
Category:Health Canada approved in 2018
Category:PMDA approved in 2014