Drug – bio-affecting and body treating compositions – Identification or warning feature – Taste or smell or chemical irritation to the eye – nose – or...
Patent
1990-09-04
1992-05-26
Friedman, S. J.
Drug, bio-affecting and body treating compositions
Identification or warning feature
Taste or smell or chemical irritation to the eye, nose, or...
514256, A61K 31505, A61K 4900
Patent
active
051166003
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to a non-injection type anti-cancer composition containing a 5-fluorouracil (5-FU) type compound as an anti-cancer component and capable of inhibiting inflammation from developing due to the 5-fluorouracil type compound, and to a method of treating a cancer.
PRIOR ART
5-FU type compounds have an excellent anti-tumor effect and are widely used as an anti-cancer agent for clinical purposes. However, it is known that 5-fluorouracil type compounds have the serious problems of frequently causing inflammation in oral cavity, digestive tract tissues and the like and inducing diarrhea after administration.
J. G. Niedzwicki et al. reported that the 5-FU activated by an in-vivo phosphorylating enzyme exhibits an anti-tumor activity in cancer cells but causes inflammation in normal tissues and that some kinds of pyrimidine compounds inhibit the activation of 5-FU due to the phosphorylating enzyme (Biochemical Pharmacology, Vol.33, No.15, pp.2383-2395, 1984).
Japanese Examined Patent Publication No.37766/1988 discloses that specific triazine compounds or pyrimidine compounds used conjointly with a 5-FU type compound can improve the anti-tumor effect of the 5-FU type compound without increase of its toxicity and side effect. The pyrimidine compounds tested for improved anti-tumor effects of 5-FU type compounds in the publication would be unlikely to augment the side effect of inflammation due to the 5-FU type compound but could not mitigate the side effect.
DISCLOSURE OF THE INVENTION
It is an object of the present invention to provide an excellent anti-cancer composition capable of effectively suppressing the occurrence of inflammation due to a 5-FU type compound present therein as an effective component.
It is another object of the invention to provide a method of treating a cancer while effectively suppressing the occurrence of inflammation due to a 5-FU type compound.
According to the present invention, there is provided a non-injection type anti-cancer composition comprising a 5-fluorouracil type compound and an oxonic acid or a pharmacologically acceptable salt thereof as effective components, the composition being capable of inhibiting the development of inflammation due to the 5-fluorouracil type compound.
We conducted extensive research on the improvements in the anti-cancer effects of 5-FU type compounds by numerous pyrimidine compounds known as an agent for improving the anti-tumor effect of 5-FU type compounds and on the effects of pyrimidine compounds of inhibiting the inflammation development due to the 5-FU type compound. Most of compounds heretofore proved to improve the anti-tumor effects of 5-FU type compounds had no or little inhibitory effect on inflammation. Our continued intensive investigations showed the unexpected fact that an oxonic acid can effectively suppress the occurrence of inflammation and diarrhea due to a 5-FU type compound with substantially no decrease in the anti-tumor effect of 5-FU type compound. Moreover, another discovery was that an oxonic acid can produce a high degree of the inflammation-inhibiting effect only when present in a non-injection type anti-cancer agent containing a 5-FU type compound. Thus it has been made possible according to the invention to suppress effectively inflammation as in digestive tract and oral cavity and diarrhea from occurring due to a 5-FU type compound with substantially no reduction in the anti-tumor effect of 5-FU type compound. Further the anti-cancer composition of the invention increases neither the toxicity of 5-FU type compound nor other side effects than inflammation. A further finding was that the combined use of specific 5-FU type compound and oxonic acid can inhibit inflammation development more effectively. The present invention has been accomplished based on these novel findings.
5-FU type compounds include various species heretofore known as anti-cancer agents which are all known for their tendency to induce a more or less degree of inflammation after administration. Speci
Fujii, deceased Setsuro
Fujii, legal heir Shinichiro
Fukushima Masakazu
Shirasaka Tetsuhiko
Takada, legal heir Kaoruko
Friedman S. J.
Otsuka Pharmaceutical Co. Ltd.
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