Efficacy of Oral Anticancer Agents for Colorectal Cancer

  title={Efficacy of Oral Anticancer Agents for Colorectal Cancer},
  author={Junichi Sakamoto and Koji Oba and Takanori Matsui and Michiya Kobayashi},
  journal={Diseases of the Colon \& Rectum},
Efficacy of Oral Anticancer Agents for Colorectal Cancer Junichi Sakamoto, M.D., Ph.D., Koji Oba, M.S., Takanori Matsui, M.D., Ph.D., Michiya Kobayashi, M.D., Ph.D. 1 Epidemiological & Clinical Research Information Management, Kyoto University Graduate School of Medicine, Kyoto, Japan 2 Department of Gastroenterological Surgery, Aichi Cancer Center, Aichi Hospital, Aichi, Japan 3 First Department of Surgery, Kochi University, Kochi, Japan 

Versatile use of Carmofur: A comprehensive review of its chemistry and pharmacology.

Carmofur has gained attention as an acid ceramidase inhibitor and as a potential lead compound against several noncancerous diseases such as coronavirus disease 2019, Krabbe disease, acute lung injury, Parkinson's disease, dementia, childhood ependymoma etc.


The analysis of the current literature data determined that further in-depth study of the pectin properties and an assessment of the link between its structure and capabilities in the aspect of creating a colon-specific drug delivery system are relevant and promising.

Metabolism, Biochemical Actions, and Chemical Synthesis of Anticancer Nucleosides, Nucleotides, and Base Analogs.

This review focuses on the chemical synthesis and biology of anticancer nucleoside, nucleotide, and base analogs that are FDA-approved and in clinical development since 2000 and explores analog syntheses as well as improved and scale-up syntheses.

Enhanced Tumor Selectivity of 5-Fluorouracil Using a Reactive Oxygen Species-Activated Prodrug Approach.

Novel 5-fluorouracil prodrugs 1a,1b selectively kill cancer cells over normal cells and are well-tolerated in mice, suggesting that the strategy described herein can extend application of chemotherapeutic drugs.

Pectin Matrix as Oral Drug Delivery Vehicle for Colon Cancer Treatment

It is suggested that multi-particulate calcium pectinate matrix is an ideal carrier to orally deliver drugs for site-specific treatment of colon cancer as crosslinking of pectin by calcium ions in a matrix negates drug release in upper gastrointestinal tract.

Genetic and pharmacological inhibition of acid ceramidase prevents asymmetric cell division by neosis[S]

It is suggested that endoreplication occurs independent of ASAH1 while neosis is ASAH 1-dependent in both prostate and lung cancer cells, suggesting a potentially powerful strategy to eliminate cells that could otherwise serve as seed populations for recurrence.

Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.

A broad overview of urea-based medicinally relevant compounds, ranging from approved drugs to recent medicinal chemistry developments, is provided, including outlines of traditional reagents and chemical procedures for the preparation of ureas.

Synthesis and Characterization of Biodegradable Hydrogels for Oral Delivery of 5-Fluorouracil Targeted to Colon: Screening with Preliminary In Vivo Studies

Investigations indicate that pectin-co-poly(MAA) hydrogel is a suitable delivery system developed for oral delivery of the drug targeted to the colon.

Evaluation of Low Molecular Weight Cross Linked Chitosan Nanoparticles, to Enhance the Bioavailability of 5-Flourouracil

5-FU loaded NPs showed a size range (198 nm-200 nm) and zeta potential (39mV to −41mV), which ensured mechanical stability and increased retention time in blood vessels by the sustained release properties of biodegradable nanocarrier drug delivery systems.



Efficacy of oral adjuvant therapy after resection of colorectal cancer: 5-year results from three randomized trials.

These observations support the use of these agents alone after resection of early-stage disease, as well as further testing of oral agents in combination with new drugs that have recently shown antitumor activity in advanced colorectal cancer.

Phase II study of oral S-1 plus irinotecan in patients with advanced colorectal cancer: Hokkaido Gastrointestinal Cancer Study Group HGCSG0302.

The objective of this study was to establish a useful chemotherapy regimen for an out-patient setting and assess the efficacy of irinotecan plus S-1 for patients with advanced colorectral cancer.

Phase II study of S-1, a novel oral fluorophyrimidine derivative, in patients with metastatic colorectal carcinoma. S-1 Cooperative Colorectal Carcinoma Study Group.

It is suggested that S-1 achieves similar responses to those of infusional 5-FU plus leucovorin and shows the potential of another biochemical modulation with easily manageable toxicity.

Phase II study of S-1, a novel oral fluoropyrimidine derivative, in patients with metastatic colorectal carcinoma

It is suggested that S-1 achieves similar responses to those of infusional 5-FU plus leucovorin and shows the potential of another biochemical modulation with easily manageable toxicity.

[Prospective controlled study on the usefulness of Carmofur as a postoperative adjuvant chemotherapy for colorectal cancer].

The above results suggest that HCFU is useful for patients with a high risk of recurrence who had advanced colon cancer (stage III b + IV), however, additional prospective studies are required to verify them.

Adjuvant therapy with oral fluoropyrimidines as main chemotherapeutic agents after curative resection for colorectal cancer: individual patient data meta-analysis of randomized trials.

The results suggest the advantage of long term o-FPs, possibly with the injection of mitomycin C, for prognosis for curatively resected colorectal cancer patients.

Five-year results of a randomized controlled trial of adjuvant chemotherapy for curatively resected colorectal carcinoma. The Colorectal Cancer Chemotherapy Study Group of Japan.

  • Medicine
    Japanese journal of clinical oncology
  • 1995
The adjuvant use of long term oral 5-FU and intermittent mitomycin C (i.v.) to improve the survival rate of patients with curatively resected rectal cancer is concluded.

Modulation of fluorouracil by leucovorin in patients with advanced colorectal cancer: evidence in terms of response rate. Advanced Colorectal Cancer Meta-Analysis Project.

  • P. Piedbois
  • Medicine, Biology
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology
  • 1992
Tumor response should not be considered a valid surrogate end point for survival in patients with advanced colorectal cancer in future trials, according to a meta-analysis performed on nine randomized clinical trials.

Phase II trial of UFT in advanced colorectal and gastric cancer.

The results suggest that oral UFT has comparable activity to standard regimes of 5-fluorouracil, and because of the convenience of oral administration is a useful therapy in the management of patients with advanced colorectal cancer.

Oral adjuvant chemotherapy with Carmofur (HCFU) for colorectal cancer: Five‐year follow‐up. Tokai HCFU Study Group—third study on colorectal cancer

A joint study was performed by the Tokai HCFU study group, which included seven institutions, to examine the value of oral administration of Carmofur (HCFU), a 5‐fluorouracil (5‐FU) derivative, for