• Alias: TAS-102
    • An orally bioavailable combination agent composed of the cytotoxic pyrimidine analog trifluridine (5-trifluoro-2’-deoxythymidine or TFT) and a thymidine phosphorylase inhibitor tipiracil hydrochloride. TFT binds to the active site of TS, thereby reducing the nucleotide pool levels required for DNA replication. It also induces DNA fragmentation and leads to the inhibition of tumor growth.
    • FDA approved for mCRC patients who have failed previous therapy with fluoropyrimidine, oxaliplatin, irinotecan, an anti-VEGF therapy, and an EGFR therapy.
    • Recommended dose: 35 mg/m2 (based on trifluridine component) twice daily on days 1 to ys 8 to 12 of a 28-day cycle
    Other topics in Targeted and Immunotherapy Agents