Is Trifluridine Tipiracil Tablets (Lonsurf) effective?

Trifluridine and tipiracil tablets (Lonsurf) is a new anti-cancer agent composed of trifluridine (FTD) and tipiracil hydrochloride (TPI). Trifluridine is the active ingredient in TAS-102 and integrates directly into cancer DNA, causing DNA dysfunction. However, when trifluridine is taken orally, it is largely degraded into its inactive form. Tipiracil prevented the degradation of trifluridine. A previously reported phase II trial of TAS-102 found an overall survival benefit in Japanese patients with refractory metastatic colorectal cancer.

In preclinical studies, trifluridine and tipiracil tablets have shown antitumor activity against cancer cell lines that are resistant to fluorouracil, the standard treatment for colorectal cancer. The patient had metastatic colorectal cancer that was refractory to all standard therapies, including wild-type KRAS tumors. Patients received TAS-102 or placebo and were directly compared. The researchers found that TAS-102 prolonged overall survival, with median overall survival being 7.1 months for TAS-102 and 5.3 months for placebo. TAS-102 also improved progression-free survival and was well tolerated, with the most common side effect being neutropenia.

The original drug of trifluridinetipiracil tablets has been marketed in China under the trade name Langsif, but it has not yet entered the scope of medical insurance. The price per box may be around RMB 6,000, and the price per box of the Hong Kong version may be more than RMB 10,000 (the price may fluctuate due to exchange rates). The Japanese version of trifluridine tipiracil tablets sold overseas may cost around more than 5,000 yuan per box (the price may fluctuate due to exchange rates). There are also cheaper generic versions of trifluridine and tipiracil tablets available overseas. Their pharmaceutical ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of each box produced by an Indian pharmaceutical factory may be around more than 1,000 yuan (the price may fluctuate due to exchange rates).