Antitumor Activities of A Novel Fluoropyrimidine, N4-Pentyloxycarbonyl-5'-deoxy-5-fluorocytidine (Capecitabine)

Capecitabine (N4-pentyloxycarbonyl-5'-fluorocytidine) is a novel fluoropyrimidine carbamate that was synthesized for the purpose of finding antitumor drugs with improved safety and efficacy profiles compared with those of 5-fluorouracil (5-FUra) and doxifluridine (5'-deoxy-5-fluorouridine,...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 1998/07/15, Vol.21(7), pp.713-717
Main Authors: ISHIKAWA, Tohru, FUKASE, Yu, YAMAMOTO, Taeko, SEKIGUCHI, Fumiko, ISHITSUKA, Hideo
Format: Article
Language:English
Subjects:
Analysis of Variance
Animals
Antimetabolites, Antineoplastic - therapeutic use
Antineoplastic agents
Antineoplastic Agents - therapeutic use
antitumor activity
Biological and medical sciences
Capecitabine
Chemotherapy
Deoxycytidine - analogs & derivatives
Deoxycytidine - therapeutic use
Female
Floxuridine - therapeutic use
Fluorouracil - therapeutic use
Humans
Male
Medical sciences
Mice
Mice, Inbred BALB C
Neoplasm Metastasis - prevention & control
novel fluoropyrimidine
Pharmacology. Drug treatments
Pyrimidines - therapeutic use
Subrenal Capsule Assay
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Summary:Capecitabine (N4-pentyloxycarbonyl-5'-fluorocytidine) is a novel fluoropyrimidine carbamate that was synthesized for the purpose of finding antitumor drugs with improved safety and efficacy profiles compared with those of 5-fluorouracil (5-FUra) and doxifluridine (5'-deoxy-5-fluorouridine, 5'-dFUrd). The present study compared the antitumor activities of the compound with those of other fluoropyrimidines in 12 human cancer xenograft models and their antimetastatic activities in murine tumor models. The antitumor efficacy of capecitabine was greater than those of 5'-dFUrd, UFT (a mixture of tegafur and uracil) and 5FUra. Capecitabine was also much safer, particularly much less toxic to the intestinal tract, than the other compounds, indicating higher therapeutic indices. The therapeutic indices. The therapeutic indices of capecitabine, 5'-dFUrd and 5-FUra were >40, >20 and 2.0 against the human CXF280 colon cancer xenograft, the most sensitive line to the fluoropyrimidines so far tested, and 5.1, 1.5, and
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.21.713