Trifluridine and tipiracil


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Company: Taiho Oncology
Approval Status: FDA Approved September 2015
Specific Treatments: metastatic colorectal cancer
Drug: Trifluridine and tipiracil



Lonsurf is a combination of trifluridine, a nucleoside metabolic inhibitor, and tipiracil, a thymidine phosphorylase inhibitor.

Lonsurf is specifically indicated for 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. 

Lonsurf is supplied as tablet for oral administration. The recommended dose is 35 mg/m2 /dose orally twice daily on Days 1 through 5 and Days 8 through 12 of each 28-day cycle. Lonsurf should be administered within 1 hour after completion of morning and evening meals. 



FDA Approval

The FDA approval of Lonsurf was based on an international, randomized, double-blind, placebo-controlled study conducted in patients with previously treated metastatic colorectal cancer. A total of 800 patients were randomized 2:1 to receive Lonsurf (N=534) plus best supportive care (BSC) or matching placebo (N=266) plus BSC. Randomization was stratified by KRAS status (wild-type vs. mutant), time since diagnosis of first metastasis (<18 months vs. ≥ 18 months), and region (Japan vs. US, Europe and Australia). Patients received 35 mg/m2 Lonsurf or matching placebo orally twice daily after meals on Days 1 – 5 and 8 – 12 of each 28-day cycle until disease progression or unacceptable toxicity. The major efficacy outcome measure was overall survival (OS) and an additional efficacy outcome measure was progression-free survival (PFS). A statistically significant improvement in overall survival and progression-free survival were demonstrated in patients in the Lonsurf plus BSC arm compared to those who received placebo plus BSC. Median OS (months) was 7.1 versus 5.3 (p<0.001). PFS was 88% versus 94%, respectively (p<0.001).



Adverse effects associated with the use of Lonsurf may include, but are not limited to, the following:

  • anemia
  • neutropenia
  • asthenia/fatigue
  • nausea
  • thrombocytopenia
  • decreased appetite
  • diarrhea
  • vomiting
  • abdominal pain
  • pyrexia



Lonsurf  is a combination of trifluridine, a nucleoside metabolic inhibitor, and tipiracil, a thymidine phosphorylase inhibitor. Following uptake into cancer cells, trifluridine is incorporated into DNA, interferes with DNA synthesis and inhibits cell proliferation. 

Source: centerwatch