Fluorouracil
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Fluorouracil
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| Systematic (IUPAC) name | |
| 5-fluoro-1H-pyrimidine-2,4-dione | |
| Identifiers | |
| CAS number | |
| ATC code | L01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C4H3FN2O2 |
| Mol. mass | 130.077 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 28 to 100% |
| Protein binding | 8 to 12% |
| Metabolism | Intracellular and hepatic |
| Half life | 10 to 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.
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[edit] Uses
The chemotherapy agent 5-FU (fluorouracil), which has been in use against cancer for about 40 years, acts in several ways, but principally as a thymidylate synthase inhibitor, interrupting the action of an enzyme which is a critical factor in the synthesis of pyrimidine-which is important in DNA replication [1].
Some of its principal use is in colorectal cancer and pancreatic cancer, in which it has been the established form of chemotherapy for decades (platinum-containing drugs are a recent addition).
[edit] 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.
[edit] 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. There are laboratory tests to determine the relative activity of the DPD enzyme, but these tests are not currently commercially available, and therefore seem to fall under the domain of research tools. Thousands of patients eagerly await the increased availability of clinical DPD testing. Work in this sector has been carried out in both the U.S. and Europe. Currently there is only one lab planning to offer DPD testing, 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.
[edit] External links
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