5-Fluorouracil: Forty-Plus and Still Ticking. A Review of its Preclinical and Clinical Development

doi:10.1023/A:1006416410198

Paper

5-Fluorouracil: Forty-Plus and Still Ticking. A Review of its Preclinical and Clinical Development

Published Nov 1, 2000 · J. Grem

Investigational New Drugs

Q1 SJR score

369

Citations

8

Influential Citations

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Abstract

Abstract5-Fluorouracil (5-FU) and 5-fluoro-2′-deoxyuridine (FdUrd) are pyrimidine analogs that have been partof the therapeutic armamentarium for a variety of solid tumorsfor over forty years. 5-FU has customarily required intravenousadministration due to poor and erratic oral bioavailability,while FdUrd has generally been employed for regionaladministration to the liver or the peritoneal cavity. A greatdeal of knowledge has been gained concerning the cellularpharmacology and mechanism of action of 5-FU since it was firstsynthesized in the late 1950's. A more thorough understanding ofthe factors influencing the metabolic activation of 5-FU and itscellular effects has generated considerable interest in combiningit with both modulatory agents such as leucovorin andmethotrexate that enhance its metabolism or cytotoxic effects.In addition, 5-FU has also been employed to enhance thetherapeutic activity of other antineoplastic agents or modalitiessuch as cisplatin and ionizing radiation with which it cansynergize. Appreciation of the clinical pharmacology of 5-FU andFdUrd have led to a variety of schedules that are clinicallyuseful. The preelinical and clinical pharmacology of 5-FU isreviewed to provide a basis for exploring the novel approachesto permit oral administration of 5-FU or its prodrugs that willbe described in other articles in this issue.

Literature Review

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Study Snapshot

5-Fluorouracil has been used for solid tumor treatment for over 40 years, with improved oral bioavailability and potential for synergistic use with other antineoplastic agents.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

5-Fluorouracil: Forty-Plus and Still Ticking. A Review of its Preclinical and Clinical Development

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References

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Oral administration of 5-fluorouracil (5-FU) is rational for patients with malignant liver tumors due to rapid absorption and higher availability in portal blood compared to systemic blood.

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Adding chemotherapy with fluorouracil and cisplatin to pelvic radiation significantly improves survival and disease-free survival in women with locally advanced cervical cancer.

Citations

Regulatory role of non-coding RNAs in 5-Fluorouracil resistance in gastrointestinal cancers

Non-coding RNAs play a crucial role in regulating 5-fluorouracil resistance in gastrointestinal cancers, potentially serving as biomarkers or therapeutic targets for this issue.

Influence of 5-Fluorination on the Structure and Glycosidic Bond Stability of the Protonated Canonical DNA and RNA Cytidine Nucleosides: Oh, What A Difference the 2′-Hydroxy Substituent Makes?

5-fluorination weakens the glycosidic bond in DNA and RNA cytidine nucleosides, with greater impact on dCyd than Cyd, but the 2′-hydroxy substituent makes a difference.

Hepatoprotective effect of Nobiletin against 5-fluorouracil induce hepatotoxicity

Nobiletin can protect against 5-florouracil-induced hepatotoxicity in male rats by decreasing apoptosis and reducing oxidative stress.

Design and fabrication of a novel platform for detection of 5-fluorouracil as the anti-cancer drug using COFs/MOFs nanocomposite with graphene quantum dotes

The modified electrode SNW-1/Cu-MOFs/GQDs/GCE effectively detects 5-fluorouracil in biological samples, with enhanced electrocatalytic performance and long-term stability.

Protein Structure Inspired Discovery of a Novel Inducer of Anoikis in Human Melanoma

Unique 3D protein structures can lead to the discovery of novel therapeutics, such as Dxr2-017, that effectively inhibit melanoma growth without harming normal cells.

The first principal study of decorated hexagonal boron nitride nanosheets with Ni and Pd atoms as drug carrier

Decorated hexagonal boron nitride nanosheets with Ni and Pd atoms show potential as efficient carriers for the anticancer medicine 5-fluorouracil, improving geometry and electronic properties for efficient cancer therapy.