5-Fluorouracil (5-FU) is a key anticancer drug that for its broad antitumor activity, as well as for its synergism with other anticancer drugs, has been used to treat various types of malignancies. In chemotherapeutic regimens, 5-FU has been combined with oxaliplatin, irinotecan and other drugs as a continuous intravenous infusion.

Fluorinated byproducts of 5-FU metabolisms, that include fluorouridine triphosphate (FUTP) and fluorodeoxyuridine triphosphate (FdUTP) may also be misincorporated into RNA and DNA of tumor cells to further disrupt protein translation and expression.

Feb 16, 2024 · Fluorouracil, also known as 5-fluorouracil or 5-FU, belongs to the class of chemotherapy drugs used to treat various neoplasms. Systemic fluorouracil is approved by the US Food and Drug Administration (FDA) for the treatment of gastric adenocarcinoma, pancreatic adenocarcinoma, breast adenocarcinoma, and colorectal adenocarcinoma.

Jul 12, 2001 · 5-Fluorouracil (5-FU), widely used for chemotherapy of colorectal carcinoma, requires intracellular anabolic conversion to cytotoxic nucleotides and exhibits a narrow therapeutic range with dose-dependent and concentration-dependent effects. 5-FU undergoes extensive metabolic degradation to several catabolites, which are excreted mainly by the ...

May 1, 2003 · 5-Fluorouracil (5-FU; see structure) is converted to three main active metabolites: fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine...

We developed and validated an HPLC method to simultaneously determine plasma concentrations of 5-FU and the three main metabolites, and we analysed the plasma concentration-time curves of the first dose of 18 colon cancer patients treated with folinic acid and 5-FU 400 mg m (-2) by intra-venous bolus injection as adjuvant chemotherapy.

Due to its structure, 5-FU interferes with nucleoside metabolism and can be incorporated into RNA and DNA, leading to cytotoxicity and cell death [5,6]. Over the past 50 years, despite its many advantages, clinical applications have been greatly limited due to drug resistance.

Oct 1, 1998 · 5-FU is eliminated primarily by hepatic metabolism, with less than 5% of the drug excreted unchanged in the urine in normal individuals. Much of the variability in 5-FU pharmacokinetics has been attributed to intra- and interindividual variation in activity of DPD, the initial and rate-limiting enzyme in 5-FU catabolism (Figure 3).

Dec 1, 2023 · This review primarily summarizes the main tumor metabolic alterations linked with 5-FU resistance and promising chemotherapy combinations, to overcome 5-FU resistance from the perspective of intervening tumor metabolism and to identify the potential for metabolic targets in tumor therapy.

Historically, both the pharmaceutical industry and academia in Japan have contributed to the development of oral 5-FU drugs. This review will summarize the current knowledge about 5-FU metabolism, and the information about orally-administrable 5-FU drugs.