Abstract
The role of oral chemotherapy has been getting expanded because of the potential advantage in patients convenience and better quality of life as well as in cost-effectiveness as compared with intravenous chemotherapy. In this article, the history, mechanism of anti-tumor activity, and clinical use of oral chemotherapy using 5-fluorouracil (5-FU) derivative chemotherapeutic agents are reviewed. Pharmacological analysis has revealed that 5-FU, a basic chemotherapeutic agent widely used against a variety of malignant tumors, shows a time dependent anti-tumor activity, and that continuous maintenance of 5-FU concentration in blood is the optimal method in 5-FU administration. UFT, a combination drug of ftorafur (tetrahydrofuranyl-5-fluorouracil, tegafur, FT) and uracil, has been developed to have potent anti-tumor activity by maintaining higher 5-FU concentration in blood and tumor tissues for a long time. FT is a pro-drug that releases 5-FU continuously, and uracil is added to inhibit degradation of the released 5-FU. Clinically, oral administration of UFT has proved to be effective as an adjuvant therapy after surgery for some malignant tumors such as non-small cell lung cancer. Moreover, UFT has proved to be effective for inoperable advanced malignancies such as colorectal cancer, especially in combination with leucovorin or cisplatin. Recently, S-1, a more active oral 5-FU derivative chemotherapeutic agent has been developed in Japan. Several factors to affect anti-tumor effects and/or toxicities of 5-FU and the derivatives, such as thymidylate synthase activity, dehydropyrimidine dehydrogenase activity and p53 status, are also discussed in the article. In conclusion, oral administration of 5-FU derivatives such as UFT may have several clinical advantages over intravenous 5-FU administration.
Keywords: 5 Fluorouracil derivative, Oral chemotherapy, Leucovorin, Cisplatin, Anti tumor effects, Toxicities
Current Pharmaceutical Biotechnology
Title: The History, Mechanism and Clinical Use of Oral 5-Fluorouracil Derivative Chemotherapeutic Agents
Volume: 1 Issue: 2
Author(s): Fumihiro Tanaka, Tatsuo Fukuse, Hiromi Wada and Masakazu Fukushima
Affiliation:
Keywords: 5 Fluorouracil derivative, Oral chemotherapy, Leucovorin, Cisplatin, Anti tumor effects, Toxicities
Abstract: The role of oral chemotherapy has been getting expanded because of the potential advantage in patients convenience and better quality of life as well as in cost-effectiveness as compared with intravenous chemotherapy. In this article, the history, mechanism of anti-tumor activity, and clinical use of oral chemotherapy using 5-fluorouracil (5-FU) derivative chemotherapeutic agents are reviewed. Pharmacological analysis has revealed that 5-FU, a basic chemotherapeutic agent widely used against a variety of malignant tumors, shows a time dependent anti-tumor activity, and that continuous maintenance of 5-FU concentration in blood is the optimal method in 5-FU administration. UFT, a combination drug of ftorafur (tetrahydrofuranyl-5-fluorouracil, tegafur, FT) and uracil, has been developed to have potent anti-tumor activity by maintaining higher 5-FU concentration in blood and tumor tissues for a long time. FT is a pro-drug that releases 5-FU continuously, and uracil is added to inhibit degradation of the released 5-FU. Clinically, oral administration of UFT has proved to be effective as an adjuvant therapy after surgery for some malignant tumors such as non-small cell lung cancer. Moreover, UFT has proved to be effective for inoperable advanced malignancies such as colorectal cancer, especially in combination with leucovorin or cisplatin. Recently, S-1, a more active oral 5-FU derivative chemotherapeutic agent has been developed in Japan. Several factors to affect anti-tumor effects and/or toxicities of 5-FU and the derivatives, such as thymidylate synthase activity, dehydropyrimidine dehydrogenase activity and p53 status, are also discussed in the article. In conclusion, oral administration of 5-FU derivatives such as UFT may have several clinical advantages over intravenous 5-FU administration.
Export Options
About this article
Cite this article as:
Tanaka Fumihiro, Fukuse Tatsuo, Wada Hiromi and Fukushima Masakazu, The History, Mechanism and Clinical Use of Oral 5-Fluorouracil Derivative Chemotherapeutic Agents, Current Pharmaceutical Biotechnology 2000; 1 (2) . https://dx.doi.org/10.2174/1389201003378979
DOI https://dx.doi.org/10.2174/1389201003378979 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
Call for Papers in Thematic Issues
Artificial Intelligence in Bioinformatics
Bioinformatics is an interdisciplinary field that analyzes and explores biological data. This field combines biology and information system. Artificial Intelligence (AI) has attracted great attention as it tries to replicate human intelligence. It has become common technology for analyzing and solving complex data and problems and encompasses sub-fields of machine ...read more
Latest Advancements in Biotherapeutics
The scope of this thematic issue is to comprehensively explore the rapidly evolving landscape of biotherapeutics, emphasizing breakthroughs in precision medicine. Encompassing diverse therapeutic modalities, the issue will delve into the latest developments in monoclonal antibodies, CRISPR/Cas gene editing, CAR-T cell therapies, and innovative drug delivery systems, such as nanoparticle-based ...read more
![](/images/wayfinder.jpg)
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Preoperative T-staging of Colorectal Cancer by Dual-energy Computed
Tomography: A Retrospective Study
Current Medical Imaging Anticancer Peptides and Proteins: A Panoramic View
Protein & Peptide Letters Epoxycarotenoids and Cancer. Review
Current Bioactive Compounds Sodium Dependent Multivitamin Transporter (SMVT): A Potential Target for Drug Delivery
Current Drug Targets Combining Oncolytic Virotherapy and Cytotoxic Therapies to Fight Cancer
Current Pharmaceutical Design The Chemopreventive and Chemotherapeutic Potentials of Tea Polyphenols
Current Pharmaceutical Biotechnology The Janus Face of Cathelicidin in Tumorigenesis
Current Medicinal Chemistry Aptamer-Mediated Cancer Gene Therapy
Current Gene Therapy Molecular Dynamics Simulations of Metalloproteinases Types 2 and 3 Reveal Differences in the Dynamic Behavior of the S1 Binding Pocket
Current Pharmaceutical Design Resveratrol, a Phytochemical Inducer of Multiple Cell Death Pathways: Apoptosis, Autophagy and Mitotic Catastrophe
Current Medicinal Chemistry LINC01836 Promotes Colorectal Cancer Progression and Functions as ceRNA to Target SLC17A9 by Sponging miR-1226-3p
Protein & Peptide Letters The Prevention of Oral Mucositis in Patients with Blood Cancers: Current Concepts and Emerging Landscapes
Cardiovascular & Hematological Agents in Medicinal Chemistry Molecular Targeted Therapies in the Management of Head and Neck Squamous Cell Carcinoma: Recent Developments and Perspectives
Anti-Cancer Agents in Medicinal Chemistry Monofunctional Platinum (PtII) Compounds – Shifting the Paradigm in Designing New Pt-based Anticancer Agents
Current Medicinal Chemistry Quinones Derived from Plant Secondary Metabolites as Anti-cancer Agents
Anti-Cancer Agents in Medicinal Chemistry Recent Progress in Studying Curcumin and its Nano-preparations for Cancer Therapy
Current Pharmaceutical Design An Overview on Inventions Related to Ginger Processing and Products for food and Pharmaceutical Applications
Recent Patents on Food, Nutrition & Agriculture HPC Analysis of Multiple Binding Sites Communication and Allosteric Modulations in Drug Design: The HSP Case Study
Current Drug Targets Polymeric Drug Delivery Approaches for Colon Targeting: A Review
Drug Delivery Letters Characterization and in vitro Cytotoxicity Evaluation of Meloxicam Loaded PEGylated Mixed Micelles Fabricated Using Quality by Design Approach
Drug Delivery Letters