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Potentiator for radiation therapy comprising pyridine derivative as active ingredient

A technology of radiation and derivatives, applied in the direction of active ingredients of heterocyclic compounds, medical preparations containing active ingredients, organic chemistry, etc., can solve problems such as development problems, and achieve the effect of reducing side effects and excellent cancer treatment effect.

Inactive Publication Date: 2011-05-04
TAIHO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the treatment of radiation-resistant tumors, it is desired to use agents that enhance radiation sensitivity in combination, but many reported radiation therapy enhancers (radiation sensitizers, etc.) have problems in development due to neurotoxicity

Method used

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  • Potentiator for radiation therapy comprising pyridine derivative as active ingredient
  • Potentiator for radiation therapy comprising pyridine derivative as active ingredient
  • Potentiator for radiation therapy comprising pyridine derivative as active ingredient

Examples

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Effect test

preparation example 1

[0080] Preparation example 1 tablet

[0081] CDHP 18mg

[0082] Starch 110mg

[0083] Magnesium Stearate 17mg

[0084] Lactose 40mg

[0085] Total 185mg

preparation example 2

[0086] With the above-mentioned compounding ratio, prepare 185 mg per tablet according to the usual method. Preparation example 2 tablet

[0087] CNDP 12mg

[0088] Lactose 54mg

[0089] Crystalline Cellulose 20mg

[0090] Magnesium Stearate 5mg

[0091] Talc 3mg

[0092] Methylcellulose 10mg

[0093] Total 104mg

[0094] With the above compounding ratio, according to the usual method, prepare each 104mg tablet formulation example 3 granules

[0095] CDHP 58mg

[0096] Lactose 340mg

[0097] Corn starch 450mg

[0098] Hydroxypropyl Methyl Cellulose 10mg

[0099] Total 858mg

[0100] Granules are prepared according to the usual method at the above-mentioned compounding ratio.

[0101] Preparation example 4 suppositories

[0102] CDHP 110mg

[0103] Witepsol W-35 900mg

[0104] Total 1010mg

[0105] With the above-mentioned compounding ratio, suppositories are prepared according to the usual method.

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Abstract

Disclosed is a potentiator for radiation therapy which can be used in combination with cancer radiation therapy to increase the radiation dose and can also reduce adverse side effects of the radiation therapy. A potentiator for radiation therapy comprising, as the active ingredient, a pyridine derivative represented by the general formula (1): (1) wherein R<1>, R<2> and R<4> independently represent a hydrogen atom, a hydroxyl group or a protected hydroxyl group, provided that all of R<1>, R<2> and R<4> are not a hydrogen atom; R<3> represents a halogen atom, an amino group, a carboxyl group, a carbamoyl group, a cyano group, a nitro group, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms or a carbonyl group having an alkoxy group having 1 to 6 carbon atoms.

Description

technical field [0001] The present invention relates to a radiotherapy enhancer, which can reduce the dose of radiation and reduce side effects when used in combination with cancer radiotherapy. Background technique [0002] Conventionally, cancer (malignant tumor) has been treated using surgery, chemotherapy, immunotherapy, thermotherapy, and radiation therapy. For various cancers such as gastric cancer, colorectal cancer, pancreatic cancer, head and neck cancer, esophageal cancer, lung cancer, and breast cancer that have progressed to stages III to IV, radiation therapy is mostly performed, but when radiation is used alone (currently clinically In the treatment with a total radiation dose of 40 to 60 Gy), long-term implementation is difficult due to hematological toxicity and digestive system side effects such as thirst, so the clinical effect (antitumor effect) is not sufficient. In order to obtain a high antitumor effect, chemoradiotherapy, which is a combination of che...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/69A61K41/00A61K31/44A61P35/00
Inventor 福岛正和
Owner TAIHO PHARMA CO LTD
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