New drugs in therapy of colorectal cancer: preclinical studies

Y M Rustum; S Cao

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New drugs in therapy of colorectal cancer: preclinical studies

Journal article

Peer reviewed

New drugs in therapy of colorectal cancer: preclinical studies

Y M Rustum and S Cao

Seminars in oncology, Vol.26(6), pp.612-620

12/1999

PMID: 10606254

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Abstract

For years, 5-fluorouracil (5-FU) was the only chemotherapeutic agent for the treatment of patients with advanced colorectal cancer. Based on laboratory data, modulation of 5-FU by leucovorin (LV) was proven to be an active alternative. In addition, a number of 5-FU prodrugs and antifolate antimetabolites became available for preclinical and clinical evaluation. With the 5-FU prodrugs, the overall aim was to improve the therapeutic efficacy and selectivity of 5-FU and to provide an oral form of therapy. In preclinical systems, several of the 5-FU prodrugs, eg, capecitabine, uracil/ ftorafur (UFT)/LV, and S- , are active and offer significant therapeutic advantages over 5-FU/LV. A direct and specific new thymidylate synthase (TS) inhibitor, Tomudex (raltitrexed, ZDI694; Zeneca Pharmaceuticals, Macclesfield, UK), is active in several preclinical and clinical settings. The major focus of this report will be on the preclinical development of selected fluoropyrimidine prodrugs.

Animals

Antimetabolites, Antineoplastic - pharmacology

Antimetabolites, Antineoplastic - therapeutic use

Capecitabine

Colorectal Neoplasms - drug therapy

Deoxycytidine - analogs & derivatives

Deoxycytidine - pharmacology

Deoxycytidine - therapeutic use

Dihydrouracil Dehydrogenase (NADP)

Drug Combinations

Drug Evaluation, Preclinical

Enzyme Inhibitors - pharmacology

Enzyme Inhibitors - therapeutic use

Fluorouracil - pharmacology

Fluorouracil - therapeutic use

Folic Acid Antagonists - pharmacology

Folic Acid Antagonists - therapeutic use

Humans

Oxidoreductases - antagonists & inhibitors

Prodrugs - pharmacology

Prodrugs - therapeutic use

Quinazolines - pharmacology

Quinazolines - therapeutic use

Tegafur - pharmacology

Tegafur - therapeutic use

Thiophenes - pharmacology

Thiophenes - therapeutic use

Thymidine Phosphorylase - antagonists & inhibitors

Thymidylate Synthase - antagonists & inhibitors

Uracil - analogs & derivatives

Uracil - pharmacology

Uracil - therapeutic use

Details

Title: Subtitle: New drugs in therapy of colorectal cancer: preclinical studies
Creators: Y M Rustum - Roswell Park Cancer Institute
S Cao
Resource Type: Journal article
Publication Details: Seminars in oncology, Vol.26(6), pp.612-620
PMID: 10606254
ISSN: 0093-7754
eISSN: 1532-8708
Grant note: CA65761 / NCI NIH HHS
Language: English
Date published: 12/1999
Academic Unit: Hematology, Oncology, and Blood & Marrow Transplantation; Internal Medicine
Record Identifier: 9984359817902771

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18 Times Cited - Web of Science