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Potentiator for radiation therapy comprising pyridine derivative as active ingredient

a technology of pyridine derivative and active ingredient, which is applied in the direction of heterocyclic compound active ingredients, drug compositions, biocides, etc., can solve the problems of long-term treatment using radiation alone, insufficient clinical effect (antitumor effect), and thought to be difficult, so as to improve the effect of cancer treatment, reduce adverse drug reactions, and reduce radiation dos

Inactive Publication Date: 2009-05-28
TAIHO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0016]Since use of the radiotherapy enhancer of the present invention and radiotherapy in combination achieves excellent cancer therapeutic effect at a lower radiation dose and reduces adverse drug reactions, long-term effective cancer treatment is enabled.

Problems solved by technology

However, long-term treatment using radiation alone (a total radiation dose of 40 to 60 Gy is currently used in clinical setting) is thought to be difficult due to adverse drug reactions in the digestive system, such as hematological toxicity and dry mouth, and its clinical effect (antitumor effect) is therefore insufficient.
However, since adverse drug reactions of chemotherapeutic drugs themselves occur in the conventional use of chemotherapeutic drugs and radiotherapy in combination, the medial practice may have to be discontinued as a result.
However, these compounds have not been used in practice due to their too severe neurotoxicity at doses at which sensitization activity can be obtained and the like.
While combination use of a drug that enhances radiation sensitivity is desired in the treatment of radiation-resistant tumors, this neurotoxicity has become problematic in the development of many of the previously reported radiotherapy enhancers (radiation sensitizers, etc.).

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

Experimental program
Comparison scheme
Effect test

preparation example 1

Tablets

[0045]

CDHP18mgStarch110mgMagnesium stearate17mgLactose40mgTotal185mg

[0046]Tablets of 185 mg / tablet were prepared with the above mixture composition according to a usual method.

preparation example 2

Tablets

[0047]

CNDP12mgLactose54mgCrystalline cellulose20mgMagnesium stearate5mgTalc3mgMethylcellulose10mgTotal104mg

[0048]Tablets of 104 mg / tablet were prepared with the above mixture composition according to a usual method.

preparation example 3

Granules

[0049]

CDHP58mgLactose340mgCorn starch450mgHydroxypropylmethylcellulose10mgTotal858mg

[0050]Granules were prepared with the above mixture composition according to a usual method.

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PUM

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Abstract

The present invention relates to a radiotherapy enhancer that can reduce the radiation dose and adverse drug reactions when used in combination with a cancer radiotherapy. There is provided a radiotherapy enhancer comprising, as an active ingredient, a pyridine derivative represented by general formula (1):wherein R1, R2, and R4 may be the same or different from one another and represent a hydrogen atom, hydroxy group, or protected hydroxy group, excluding the case where R1, R2, and R4 are all a hydrogen atom, and R3 represents a halogen atom, amino group, carboxyl group, carbamoyl group, cyano group, nitro group, alkyl group having 1 to 6 carbon atoms, alkenyl group having 2 to 6 carbon atoms, or carbonyl group containing an alkoxy group having 1 to 6 carbon atoms).

Description

TECHNICAL FIELD[0001]The present invention relates to a radiotherapy enhancer that can reduce the radiation dose and adverse drug reactions, when used in combination with cancer radiotherapy.BACKGROUND ART[0002]Conventionally, surgical therapy, chemotherapy, immunotherapy, thermotherapy, and radiotherapy have been performed for the treatment of cancer (malignant tumor). Radiotherapy is often performed for various types of cancers such as gastric cancer, colorectal cancer, pancreatic cancer, head and neck cancer, esophageal cancer, lung cancer, and breast cancer that are advanced to stage III or IV. However, long-term treatment using radiation alone (a total radiation dose of 40 to 60 Gy is currently used in clinical setting) is thought to be difficult due to adverse drug reactions in the digestive system, such as hematological toxicity and dry mouth, and its clinical effect (antitumor effect) is therefore insufficient. To achieve a high antitumor effect, chemoradiotherapy using chem...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/44C07D213/69A61P35/00
CPCC07D213/69A61K41/0038A61P35/00A61K31/44
Inventor FUKUSHIMA, MASAKAZU
Owner TAIHO PHARMA CO LTD
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