Small molecule
PubChem CID 3385
Fluorouracil
Adrucil
- Mechanism of action
- Thymidylate synthase inhibitor (antimetabolite)
- In plain language
- Blocks the enzyme cancer cells need to build new DNA, so damaged cells can't copy themselves and die off.
- How it works
- Fluorouracil is a fluorinated pyrimidine analog that is metabolized intracellularly to active forms, principally FdUMP, which forms a stable ternary complex with thymidylate synthase and a folate cofactor, blocking de novo synthesis of thymidine and thereby depleting the deoxythymidine triphosphate pool required for DNA replication and repair. Other active metabolites are misincorporated directly into DNA and RNA, disrupting nucleic acid processing and function. The combined effect of thymidylate depletion and fraudulent nucleotide incorporation preferentially damages rapidly proliferating cells, driving cytotoxicity in tumor tissue.
- Therapeutic applications
- Indicated for the treatment of adenocarcinoma of the colon and rectum, adenocarcinoma of the breast, gastric adenocarcinoma, and pancreatic adenocarcinoma, used palliatively, generally as part of combination chemotherapy regimens, in patients considered incurable by surgery or other means.
- Class
- Small molecule
- Therapeutic area
- Oncology
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