TAS-102 is a combination of two active ingredients: trifluridine (TFT), a nucleoside analog, and tipiracil (TPI), a thymidine phosphorylase inhibitor in a 1.0:0.5 molar ratio (TFT:TPI).1 TFT is the active antitumor component of TAS-102, its monophosphate form inhibits thymidylate synthase, an enzyme that plays a main role in DNA synthesis, and its triphosphate form is incorporated into DNA in tumor cells resulting in DNA dysfunction. TPI increases the bioavailability of TFT that is rapidly degraded to its inactive form by thymidine phosphorylase in the intestines and liver. The formulation presents a double targeted due to the cytotoxic effect of TFT, which is enhanced by TPI, while TPI also exerts antiangiogenic effects by inhibiting thymidine phosphorylase.2 TAS 102 inhibits KM20C colon cancer xenograft growth by 70.5% when was orally administered twice daily at a dose of 150 mg/kg for 14 days.3 TAS-102 has great potential to improve the treatment of malignancies when combined with other angiostatic or cytotoxic agents. A combination of TAS-102 and Avastin, an antineoplastic agent, was found to increase chemotherapeutic efficacy against colorectal cancer xenograft, compared with that for either drug alone.4
Biochem/physiol Actions
Anti cancer, Anti angiogenic
Other Notes
Solubility:DMSO 100 mg/mL; water 15mg/ml TAS-102 is a mixture of 2 components. In order to maintain the original ratio between the components, the entire content of vial needs to be solubilized.
