trifluridine + tipiracil + temozolomide

Trifluridine + tipiracil + temozolomide is a combination chemotherapy regimen being investigated for the treatment of metastatic pancreatic neuroendocrine tumors (pNETs). The regimen consists of TAS-102 (a fixed-dose combination of the nucleoside analog trifluridine and the thymidine phosphorylase inhibitor tipiracil) and the alkylating agent temozolomide. Trifluridine exerts its antineoplastic effect by inhibiting thymidylate synthase and incorporating into DNA, while tipiracil prevents the rapid degradation of trifluridine by inhibiting thymidine phosphorylase, thereby increasing its systemic exposure. Temozolomide contributes to the regimen's efficacy by methylating DNA, leading to DNA damage and apoptosis. This combination is currently being evaluated in a Phase 1B clinical trial (NCT02943733) sponsored by the University of Wisconsin, Madison, to determine the maximum tolerated dose and safety profile in patients with advanced pNETs who may be resistant to other fluoropyrimidine agents.

Brand names

LonsurfTemodar

Other names

TAS-102 + temozolomideLonsurf + TemodarA-University of Wisconsin, Madison-pancreatic neuroendocrine tumor