Trifluridine and tipiracil (Lonsurf)
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.
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Diseases for which it is used
Patient drug information
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. (Based on RECOURSE)
- 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; based on TAGS)
Also known as
- Code name: TAS-102
- Generic names: trifluridine/tipiracil, trifluridine & tipiracil
- Brand name: Lonsurf