The application of trifluridine and tipiracil (Lancever) in colon cancer

Trifluridine and tipiracil (Lonsurf) were approved in 2015 for patients with advanced (metastatic) colorectal cancer who have no longer responded to other treatments, such as certain chemotherapy and biological therapies. In August 2023, trifluridine tipiracil combined with bevacizumab was approved for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have previously received other therapies but no longer responded. Trifluridine and tipiracil are classified as nucleoside metabolism inhibitors that incorporate directly into DNA and interfere with its function. Blood levels of trifluridine are maintained by the enzyme inhibitor tipiracil.

In a colorectal cancer clinical study of trifluridine tipiracil alone, half of the patients treated with trifluridine tipiracil tablets survived 7.1 monthsHalf of the patients treated with placebo survived 5.3 months, a statistically significant result. Patients in the trifluridine-tipiracil group survived from 6.5 months to 7.8 months, compared with 4.6 months to 6 months in the placebo group. On average, patients treated with trifluridine-tipiracil took 2 months to develop their cancer, and 88% experienced disease progression or death.

In the phase 3 SUNLIGHT trial, when trifluridine-tipiracil was combined with bevacizumab, half of the patients with metastatic colorectal cancer lived 10.8 months, compared with only 7.5 months in the trifluridine-tipiracil group, a 39% reduction in the risk of death. In this study, progression-free survival (PFS) was 5.6 months for half of the patients who received trifluridine plus bevacizumab, compared with 2.4 months for those who received trifluridine and bevacizumab alone. This resulted in a 56% relative risk reduction in disease progression.