TAS-102 (Lonsurf)
Other Medications · Approved since 2015
Description
TAS-102 (trifluridine/tipiracil) is an oral nucleoside antimetabolite chemotherapy agent approved for the treatment of metastatic colorectal cancer in patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, anti-VEGF therapy, and anti-EGFR therapy (if RAS wild-type). This combination drug consists of trifluridine, a thymidine-based nucleoside analog, and tipiracil, a thymidine phosphorylase inhibitor that prevents degradation of trifluridine. TAS-102 provides a treatment option for heavily pretreated patients with refractory metastatic colorectal cancer who have exhausted standard therapeutic options.
Mechanism of Action
Trifluridine is incorporated into DNA after phosphorylation to its active triphosphate form, causing DNA dysfunction and ultimately cell death. Tipiracil enhances the antitumor activity by inhibiting thymidine phosphorylase, thereby maintaining higher concentrations of trifluridine in plasma and tumor tissues.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.