TAS102

Description

TAS-102 (trifluridine/tipiracil, brand name Lonsurf) is an oral chemotherapy combination approved for the treatment of metastatic colorectal cancer (mCRC) in patients who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF agent, and if RAS wild-type, an anti-EGFR agent. Its approval was supported by the pivotal RECOURSE trial, which demonstrated a significant improvement in overall survival (OS) compared to placebo (7.1 vs. 5.3 months; HR 0.68). TAS-102 is typically used as a third-line or later treatment option and may also be combined with bevacizumab, as supported by the SUNLIGHT trial, which showed improved OS (10.8 vs. 7.5 months) in the combination arm. It represents an important option for patients with refractory mCRC regardless of RAS, BRAF, or MSI status.

Mechanism of Action

Trifluridine is a nucleoside analog that is incorporated directly into DNA during replication, causing DNA dysfunction and cell death; this mechanism is distinct from that of 5-fluorouracil. Tipiracil is a thymidine phosphorylase inhibitor that prevents the rapid degradation of trifluridine, thereby maintaining its therapeutic plasma concentrations.

Molecular Targets

Side Effects

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials