Synonyms: TFT | trifluorothymidine
trifluridine is an approved drug (Japan, FDA (2015), EMA (2016))
Compound class:
Synthetic organic
Comment: Trifluridine was originally approved by the US FDA in 1980, and was used for its antiviral effects (marketed as Vitroptic®). The drug is now being investigated for its antineoplastic (cytotoxic) effect.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Trifluridine is a component of the anticancer therapeutic Lonsurf® (code-named TAS-102), that was first approved in Japan for the treatment of metastatic/unresectable colorectal cancer. The other component of TAS-102 is tipiracil [1]. In September 2015, the US FDA approved Lonsurf® for the treatment of patients with RAS wild type, metastatic colorectal cancer who have already received chemotherapy, anti-VEGF, and anti-EGFR therapies. Lonsurf® was EMA approved in 2016. TAS-102 is being assessed in Phase 3 clinical trial for metastatic gastric cancer (NCT02500043). |
Mechanism Of Action and Pharmacodynamic Effects |
Trifluridine is a modified form of deoxyuridine (nucleoside analogue). Trifluridine is metabolised to its monophosphate-derivative and this inhibits thymidylate synthase, one of the rate-limiting enzymes in pyrimidine de novo deoxynucleotide synthesis. Thymidylate synthase is therefore crucial for DNA synthesis. In addition, if trifluridine is incorporated directly in to DNA during replication, the -CF3 group of trifluridine blocks base pairing. These actions underly the compound's cytotoxic effect [2]. |
External links |
For extended ADME data see the following: Drugs.com |