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.
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.

Diseases for which it is used

• Colon cancer
• Gastric cancer

Patient drug information

• Trifluridine and tipiracil (Lonsurf) package insert

History of changes in FDA indication

• 9/22/2015: 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.
• 2/22/2019: 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)

Also known as

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