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.[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
- 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