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Modified hydroxypolymer conjugates with bone seeking and tumor killing moieties

A technology of hydroxyl polymers and modified hydroxyl groups, which is used in medical preparations of non-active ingredients, antineoplastic drugs, drug combinations, etc.

Active Publication Date: 2011-03-23
DEXTECH MEDICAL AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some patients experience long-term pain relief, however, many patients continue to experience pain despite treatment

Method used

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  • Modified hydroxypolymer conjugates with bone seeking and tumor killing moieties
  • Modified hydroxypolymer conjugates with bone seeking and tumor killing moieties
  • Modified hydroxypolymer conjugates with bone seeking and tumor killing moieties

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis of Dextran-guanidine-bisphosphonate

[0039] activation

[0040] Pharmaceutical grade dextran PM40 (150 mg) was dissolved in 5 ml of water. 120 mg of sodium periodate was added, followed by 25 μl of concentrated sulfuric acid. The mixed solution was stirred for 45 min. 25 [mu]l of ethylene glycol was added to stop the oxidation and destroy excess periodate by further reacting for 15 min. Then, the pH was adjusted to pH 6,5 with 0.2M sodium acetate.

[0041] Conjugate

[0042] 2 ml of the material obtained by the above method is mixed with 20 mg of alendronate and 5 mg of sodium cyanoborohydride. The solution was stirred and incubated for 1.5 hours at room temperature. After 1.0 hour, 80 mg of aminoguanidine was added. The solution was stirred for a further 4 hours at room temperature and then separated from low molecular weight components on a PD 10 column using PBS as eluent. Obtain 4 mL of purified conjugation solution. Typically, the synthesis yiel...

Embodiment 2

[0048] Synthesis of Dextran-guanidine-bisphosphonate

[0049] activation

[0050] Pharmaceutical grade dextran PM70 (150 mg) was dissolved in 6 ml of water. 120 mg of sodium periodate was added, followed by 25 μl of concentrated sulfuric acid. The mixed solution was stirred for 30 min. 75 [mu]l of ethylene glycol was added to stop the oxidation and destroy the excess periodate by further reacting for 15 min. Activated dextran was purified by gel filtration in 1 ml fractions on a PD-10 column using 0.1 M acetate pH 6.5 as eluent to remove low molecular weight components. In each separation, 2 ml of activated dextran solution was obtained.

[0051] conjugation mode 1

[0052] 1 ml of the eluate obtained by the above method was mixed with 10 mg of alendronate and 5 mg of sodium cyanoborohydride. The solution was stirred and incubated for 2 hours at room temperature. After 2 hours, 65 mg of 2-aminoguanidine was added. The solution was stirred overnight at room temperature ...

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Abstract

The present inven tion is related to a modified hydroxypolymer conjugate, preferably a dextran-guanidine-biphosphonate conjugate for treating not only skeletal tumors i.e. bone metastasis, particularly bone metastasis related to hormone refractory prostate cancer HRPC and breast cancer, but also osteoporosis. A method for producing and using said hydroxypolymer conjugate is also disclosed.

Description

[0001] technical field of invention [0002] The present invention relates to modified hydroxypolymer conjugates substituted with an osteophilic moiety and a tumor-killing moiety including anti-osteoclastic activity. The modified hydroxy polymer conjugate is used as a drug for treating bone cancer, osteoporosis and the like. The hydroxypolymer dextran conjugate is particularly useful in the treatment of metastatic bone lesions in refractory prostate cancer. The present invention also relates to a method for preparing the hydroxyl polymer conjugate and its use. Background of the invention [0003] Hydroxypolymers are a group of sugar polymers having a large number of hydroxyl groups which can be conveniently substituted with different moieties of effective compounds. Dextran is one of the most commonly used hydroxyl polymers in the pharmaceutical industry with established pharmaceutical uses such as prevention of hypovolemic shock, prevention of embolism and improvement of mi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K51/06A61P35/00
CPCA61K51/065A61K47/481A61K47/4823A61K47/48084A61K47/548A61K47/55A61K47/61A61P19/08A61P19/10A61P35/00A61P35/04
Inventor A·霍尔姆伯格
Owner DEXTECH MEDICAL AB
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