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Antitumor effect potentiator and antitumor agent

An anti-tumor agent and anti-tumor technology, which can be applied in the directions of anti-tumor drugs, active ingredients of heterocyclic compounds, and medical preparations of non-active ingredients, and can solve the problems of high anti-tumor activity and so on.

Inactive Publication Date: 2006-04-19
TAIHO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the combination of tegafur and uracil is known to have greater antitumor activity than tegafur alone

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Cubic fragments of human colon cancer cell line KM20C with a diameter of about 2 mm were subcutaneously transplanted into the back of male nude mice BALB / c-nu / nu. When the average tumor volume (= major axis (mm) × minor axis (mm) 2 ) to about 200mm 3 , the mice were divided into groups.

[0068] Each of the following preparations was dissolved or suspended in 0.5% hydroxypropylmethylcellulose (HPMC) solution, and the amount shown in Table 1 was orally administered to the mice once a day, and the administration was continued after grouping Day 9: Calcium folinate; Tegafur / Gimerast / Oxonate Potassium combination agent (tegafur:Gimerast:Oxonate Potassium molar ratio=1:0.4:1); A combined medicament of fluoride / gemast / oxonate potassium combined medicament and calcium folinate; a combined medicament of tegafur / uracil (the molar ratio of tegafur:uracil=1:4); and A combination of fluoride / uracil combination and folinate.

[0069] The ratio of the tumor volume 10 days after g...

Embodiment 2

[0075] Cubic fragments of human colon cancer cell line Colon 38 with a diameter of about 2 mm were subcutaneously transplanted into the back of male mice C57BL / 6. When the average tumor volume (= major axis (mm) × minor axis (mm) 2 ) to about 150mm 3 , the mice were divided into groups.

[0076] Each of the following preparations was dissolved or suspended in 0.5% hydroxypropylmethylcellulose (HPMC) solution, and the amount shown in Table 2 was orally administered to the mice once a day, and the administration was continued after grouping Day 9: Calcium folinate; Tegafur / Gimerast / Oxonate Potassium combination agent (tegafur:Gimerast:Oxonate Potassium molar ratio=1:0.4:1); Combination medicaments of fluoride / gemostat / potassium oxonate and calcium folinate; combination medicaments of tegafur / uracil (ratio of tegafur:uracil=1:4); and combinations containing the above-mentioned tegafur A combination of fluoro / uracil combination and folinate.

[0077] The ratio of the tumor vol...

Embodiment 3

[0084] Cubic fragments of human colon cancer cell line KM20C with a diameter of about 2 mm were subcutaneously transplanted into the back of male nude mice (BALB / cA-nu). When the average tumor volume (= major axis (mm) × minor axis (mm) 2 ) to about 200mm 3 , the mice were divided into groups.

[0085] Dissolve the combination agent containing tegafur / gimerast / oxonate potassium (the molar ratio of tegafur: gimonast: oxonate potassium=1:0.4:1) and calcium folinate or Suspended in 0.5% hydroxypropylmethylcellulose (HPMC) solution, and administered orally to mice once a day in the amount shown in Table 3, for 14 consecutive days from grouping.

[0086] The ratio of the tumor volume 15 days after grouping to the tumor volume at the time of grouping was calculated to obtain the relative tumor volume. The tumor growth inhibition rate (%) can be determined using the relative tumor volumes of the drug-treated group and the control group.

[0087] The change in body weight can be c...

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PUM

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Abstract

It is intended to provide: an antitumor effect potentiator containing a therapeutically efficacious amount of Tegafur, Gimeracil in an amount efficacious for potentiating the antitumor effect and Oteracil potassium in an amount efficacious in inhibiting side effects, characterized by containing at least one component selected from the group consisting of folinic acid and its pharmaceutically acceptable salts in an amount efficacious for potentiating the antitumor effect as the active ingredient; an antitumor agent characterized by containing a therapeutically efficacious amount of Tegafur, Gimeracil in an amount efficacious for potentiating the antitumor effect and Oteracil potassium in an amount efficacious in inhibiting side effects and , together with at least one component selected from the group consisting of folinic acid and its pharmaceutically acceptable salts in an amount efficacious for potentiating the antitumor effect as the active ingredient; a method of potentiating the antitumor effect of an antitumor agent characterized by comprising administering the above-described antitumor effect potentiator to a patient; and a method of treating cancer characterized by comprising administering the above antitumor agent to a patient.

Description

technical field [0001] The present invention relates to an antitumor effect enhancer and an antitumor agent. Background technique [0002] Research and development of antineoplastic agents are very active. Various effective antineoplastic agents are used clinically to treat malignant tumors. [0003] For example, tegafur is a drug that activates in vivo and releases the active form, 5-fluorouracil (hereinafter referred to as "5-FU"), and is known as an improved antineoplastic agent with less toxicity and side effects than 5-FU. Furthermore, the combination of tegafur and uracil is known to have greater antitumor activity than tegafur alone. In particular, a combination of tegafur and uracil in a molar ratio of 1:4 is commercially available in the form of capsules and granules (trademark: UFT, manufactured by Taiho Pharmaceutical Co., Ltd.). Because uracil itself has no anti-tumor activity, but inhibits the inactivation of 5-FU, which is rapidly metabolized and inactivated...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/519A61K47/22A61K31/53
CPCC07D239/553A61K31/519A61K31/53A61K31/44A61K31/513A61P13/08A61P13/10A61P35/00A61P43/00A61K47/22C07D487/04
Inventor 内田淳二首藤光洋
Owner TAIHO PHARMA CO LTD
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