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What is the primary mechanism of action for 5-Fluorouracil (5-FU) in cancer treatment?
What is the primary mechanism of action for 5-Fluorouracil (5-FU) in cancer treatment?
- Inhibition of thymidylate synthase (TS) (correct)
- Interference with microtubule formation
- Direct alkylation of DNA
- Inhibition of topoisomerase
Besides inhibiting TS, through which other mechanism does 5-FU exert its anticancer effects?
Besides inhibiting TS, through which other mechanism does 5-FU exert its anticancer effects?
- Activation of apoptosis pathways
- Interference with protein synthesis
- Direct inhibition of DNA replication
- Incorporation of its metabolites into RNA and DNA (correct)
Which of the following is a key active metabolite of 5-Fluorouracil (5-FU)?
Which of the following is a key active metabolite of 5-Fluorouracil (5-FU)?
- Fluorouracil diphosphate (FdUDP)
- Fluorouracil cytidine (FdC)
- Fluoro-deoxyuridine monophosphate (FdUMP) (correct)
- Fluorouracil triphosphate (FdUTP)
Where does the extensive metabolism of 5-FU primarily occur in the body?
Where does the extensive metabolism of 5-FU primarily occur in the body?
What is the mechanism by which capecitabine, a prodrug of 5-FU, is activated?
What is the mechanism by which capecitabine, a prodrug of 5-FU, is activated?
Flashcards
5-Fluorouracil (5-FU)
5-Fluorouracil (5-FU)
An anticancer drug used mainly for colorectal cancer.
Mechanism of 5-FU
Mechanism of 5-FU
Inhibits thymidylate synthase and incorporates into RNA/DNA.
Active metabolites of 5-FU
Active metabolites of 5-FU
Includes Fluoro-deoxyuridine monophosphate (FdUMP) among others.
5-FU metabolism
5-FU metabolism
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5-FU prodrugs
5-FU prodrugs
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Study Notes
5-Fluorouracil (5-FU)
- Widely used, particularly for colorectal cancer
- 5-FU inhibits thymidylate synthase (TS)
- 5-FU incorporates its metabolites into RNA and DNA
- 5-FU is converted to active metabolites, including Fluoro-deoxyuridine monophosphate (FdUMP)
- 5-FU is extensively metabolised in the gut and liver
- 5-FU prodrugs, like Capecitabine, are developed for oral administration
- Capecitabine is activated by a cascade of 3 enzymes into 5-FU
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