Article: Fluorouracil

Fluorouracil
Systematic (IUPAC) name
5-fluoro-1H-pyrimidine-2,4-dione
Identifiers
CAS number	51-21-8
ATC code	L01BC02
PubChem	3385
DrugBank	APRD00516
Chemical data
Formula	C4H3FN2O2
Mol. weight	130.077 g/mol
Pharmacokinetic data
Bioavailability	28-100%
Protein binding	8-12%
Metabolism	Intracellular and hepatic
Half life	10-20 minutes
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	topical and injection

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, diarrhea 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 5Fu it is relatively easy to determine the deficiency and in some case alter medication to give better results.

Work on 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 5Fu (Coventry Diagnostics) - It is expected that with a potential 500,000 people in North America using the pyrimidine based 5Fu this form of testing will increase.

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