Fluorouracil

Fluorouracil (5-FU) is a drug that is used in the treatment of cancer. It belongs to the family of drugs called antimetabolites. It is a pyrimidine analog.

Uses

Its principal use is in colorectal cancer, in which it has been the established form of chemotherapy for decades (platinum-containing drugs are a recent addition).

Mode of Action

As a pyrimidine analogue, it is transformed inside the cell into different cytotoxic metabolites which are then incorporated into DNA and RNA, finally inducing cell cycle arrest and apoptosis by inhibiting the cell's ability to synthesize DNA. It is an S-phase specific drug and only active during certain cell cycles.

Capecitabine is a prodrug that is converted into 5-FU in the tissues. It can be administered orally.

Adverse effects

Side effects include myelosuppression, mucositis, dermatitis, diarrhoea and cardiac toxicity.

When using a pyrimidine-based drug, all users must be aware that there is a genetic inability to metabolize them. Current theory points to nearly 8% of the population suffering what is termed DPD deficiency. For 5-FU it is relatively easy to determine the deficiency and in some cases alter medication to give better results.

Work in this sector has been carried out in both the US and Europe. Currently there is only one lab offering a diagnostics determination test for 5-FU incompatibility, Coventry Diagnostics. It is expected that with a potential 500,000 people in North America using the pyrimidine-based 5-FU, this form of testing will increase.

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