Target intelligence / Profile preview

Fluorouracil (5-Fluorouracil) (5-FU)

Target
5-FU
Molecular classification
Antimetabolite
01

Overview

Fluorouracil (5-FU) is not a therapeutic target such as a receptor, enzyme, or transporter. It is itself a drug—an antimetabolite chemotherapeutic agent. The query asks about "target molecule/receptor," but fluorouracil is not a target; it acts on cellular targets such as thymidylate synthase and DNA/RNA synthesis pathways. Therefore, this entry does not fit the intended use of "target" in drug discovery or pharmacology.

Other names
5-Fluoropyrimidine-2,4(1H,3H)-dioneEfudexAdrucilFluracilFU
02

Mechanism of action

Fluorouracil (5-FU) is a pyrimidine analog antimetabolite. It is converted intracellularly to several active metabolites, including fluorodeoxyuridine monophosphate (FdUMP), which inhibits thymidylate synthase (TS), leading to depletion of thymidine nucleotides and disruption of DNA synthesis. Fluorouridine triphosphate (FUTP) is incorporated into RNA, interfering with RNA processing and function. Fluorodeoxyuridine triphosphate (F-dUTP) can be incorporated into DNA, leading to DNA damage and fragmentation. These actions collectively disrupt nucleic acid synthesis and function, causing cell cycle arrest and apoptosis, particularly in rapidly proliferating cells.

03

Biological functions

Cell proliferation inhibitionDNA synthesis inhibitionRNA function interference
04

Disease associations

Cancer (colorectal cancer, breast cancer, gastric cancer, head and neck cancer, pancreatic cancer)Actinic keratosisBasal cell carcinoma
05

Safety considerations

MyelosuppressionMucositisDiarrheaHand-foot syndromeNeurotoxicityCardiotoxicitySevere toxicity in DPYD deficient patients
06

Interacting drugs

Leucovorin

10 more in the full profile.

07

Biomarkers

DPYD (Dihydropyrimidine dehydrogenase) deficiency (pharmacogenomic marker for toxicity prediction)

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