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Trifluridine


Mechanism of action:

Trifluridine is a pyrimidine nucleoside analog. After entering the cell, it is progressively phosphorylated by enzymes such as thymidine kinase into active monophosphate and triphosphate derivatives. The monophosphate form of trifluridine inhibits thymidylate synthase, blocking the formation of dTMP and causing a shortage of thymidylate required for DNA synthesis. The triphosphate form can be directly incorporated into newly synthesized DNA, resulting in DNA structural instability and ultimately causing cells or viruses to lose their capacity for replication.

Reference(s):

1. Carmine AA et al. (1982). Trifluridine: a review of its antiviral activity and therapeutic use in the topical treatment of viral eye infections. Drugs. 


2. Burness CB et al. (2016). Trifluridine/Tipiracil: A Review in Metastatic Colorectal Cancer. Drugs. 


3. Matsuoka K et al. (2018). Trifluridine/tipiracil overcomes the resistance of human gastric 5-fluorouracil-refractory cells with high thymidylate synthase expression. Oncotarget.

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