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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
4
|
| pubmed:dateCreated |
1998-12-9
|
| pubmed:abstractText |
S-1 is a new oral formulation of 5-fluorouracil (5-FU) consisted of 1M tegafur, 0.4M 5-chloro-2,4-dihydroxypyridine that inhibits a degradation of 5-FU, and 1M potassium oxonate that regulates the phosphorylation of 5-FU in the gastrointestinal tract, and has shown excellent antitumor efficacy against various murine tumors in rodents, compared to the oral tegafur-based antitumor drug, UFT (1M tegafur plus 4M uracil), which is used clinically in Japan. To assess the possibility of clinically using S-1, we investigated the antitumor effect of S-1 on various human solid tumor xenografts in athymic rats and mice. In the nude rat system, S-1 was significantly effective against all 12 tumor xenografts tested when its minimum toxic dose (15 mg/kg) was administered for 14 days. Three tumors, stomach (H-81), colon (KM12C) and breast (H-31) markedly regressed in response to treatment with S-1 but not with UFT. The antitumor potency of S-1 was weak against human tumors xenografted into nude mice and likely similar to that of UFT. The reason of the discrepancy in the efficacy of S-1 between rats and mice was found to be that the 5-FU levels in the blood and tumor tissue of rats after oral administration of S-1 persisted much longer than in mice, and this prolonged maintenance of plasma 5-FU levels was significantly related to the potent antitumor activity of S-1. In conclusion, the results of this study suggested that based on its biological and pharmacokinetic characteristics, oral S-1 should be active against various human cancers.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antimetabolites, Antineoplastic,
http://linkedlifedata.com/resource/pubmed/chemical/Drug Combinations,
http://linkedlifedata.com/resource/pubmed/chemical/Fluorouracil,
http://linkedlifedata.com/resource/pubmed/chemical/Oxonic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridines,
http://linkedlifedata.com/resource/pubmed/chemical/S 1 (combination),
http://linkedlifedata.com/resource/pubmed/chemical/Tegafur
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Oct
|
| pubmed:issn |
1019-6439
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
13
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
693-8
|
| pubmed:dateRevised |
2004-11-17
|
| pubmed:meshHeading |
pubmed-meshheading:9735397-Administration, Oral,
pubmed-meshheading:9735397-Animals,
pubmed-meshheading:9735397-Antimetabolites, Antineoplastic,
pubmed-meshheading:9735397-Drug Combinations,
pubmed-meshheading:9735397-Fluorouracil,
pubmed-meshheading:9735397-Humans,
pubmed-meshheading:9735397-Mice,
pubmed-meshheading:9735397-Mice, Inbred BALB C,
pubmed-meshheading:9735397-Mice, Nude,
pubmed-meshheading:9735397-Neoplasm Transplantation,
pubmed-meshheading:9735397-Neoplasms, Experimental,
pubmed-meshheading:9735397-Oxonic Acid,
pubmed-meshheading:9735397-Pyridines,
pubmed-meshheading:9735397-Rats,
pubmed-meshheading:9735397-Rats, Inbred F344,
pubmed-meshheading:9735397-Rats, Nude,
pubmed-meshheading:9735397-Species Specificity,
pubmed-meshheading:9735397-Tegafur,
pubmed-meshheading:9735397-Transplantation, Heterologous,
pubmed-meshheading:9735397-Treatment Outcome,
pubmed-meshheading:9735397-Tumor Cells, Cultured
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Preclinical antitumor efficacy of S-1: a new oral formulation of 5-fluorouracil on human tumor xenografts.
|
| pubmed:affiliation |
Cancer Research Laboratory-2, Hanno-City, Saitama 357, Japan.
|
| pubmed:publicationType |
Journal Article
|