Trifluridine

Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors^[1][2][3][4]. In Vitro:Trifluridine (0.5 μΜ, 3 days) induces cellular senescence in HUVECs^[2].
Trifluridine (0.5 μΜ, 3 days) inhibits autophagy and autophagy flux via the mTOR pathway in HUVECs ^[2].
Trifluridine (0-5 μΜ, 3 days) inhibits HUVEC cells viability in a concentration-dependent way^[2].
Trifluridine (5 µM-20 µM, 24 h–72 h) inhibits the proliferation in MCF-7, MDA-MB-231, BT-549 and Hs578T^[4].
Trifluridine (0 µM-20 µM, 48 h) selectively induces apoptosis in MCF-7, MDA-MB-231, BT-549 and Hs578T cells ^[4].
Trifluridine (10 µM, 72 h) induces DNA double-strand break in MCF-10A, MCF-7, MDA-MB-231 and BT-549 cells^[4].
In Vivo:Trifluridine/tipiracil (200 mg/kg, PO, twice daily for 5 consecutive days followed by 2 drug-free days for 6 weeks) shows antitumor activity in the human colorectal intraperitoneal xenograft model^[3].
Trifluridine (75 or 150 mg/kg, oral gavage, once daily for 5 consecutive days) inhibits the growth in implanted mouse TNBC tumors ^[4].