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Polyethylene glycol-dipeptide-antitumour drug complex and use thereof

An anti-tumor drug, polyethylene glycol technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of reducing the half-life of conjugates, limited effect, etc.

Inactive Publication Date: 2013-10-23
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the conjugate formed by dipeptide-conjugated monoclonal antibody and anti-tumor drug may cause an immune response in the body and reduce the half-life of the conjugate in plasma, so the effect is limited

Method used

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  • Polyethylene glycol-dipeptide-antitumour drug complex and use thereof
  • Polyethylene glycol-dipeptide-antitumour drug complex and use thereof
  • Polyethylene glycol-dipeptide-antitumour drug complex and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation of the activated PEG-X-Y of embodiment 1, X-Y is Val-Cit

[0038] Synthesized by conventional amide condensation reaction, the easily available mPEG-NHS (the average molecular weight of PEG is 4kD) and the dipeptide (Val-Cit) according to the feeding ratio of 2:1, adding pH7.5 phosphate, HEPES or Tris-HCl and other buffer solutions were dissolved, the reaction temperature was 25° C., stirred slowly for 60 minutes, and 5 times the molar amount of PEG of glycine was added to terminate the reaction. The mPEG-Val-Cit molecular complex can be obtained after dialysis purification and lyophilization. Then use conventional EDC and NHS reagents to activate the terminal carboxyl group of the mPEG-Val-Cit molecular complex to obtain mPEG-Val-Cit-NHS.

Embodiment 2

[0039] The preparation of the activated PEG-X-Y of embodiment 2, X-Y is Ala-Lys

[0040] Synthesized by conventional amide condensation reaction, the readily available mPEG-NHS and dipeptide (Ala-Lys) are dissolved in buffers such as phosphate, HEPES or Tris-HCl at pH 7.5 at a feed ratio of 2:1 , the reaction temperature was 25° C., the mixture was stirred slowly for 60 minutes, and glycine with 5 times the molar amount of PEG was added to terminate the reaction. The mPEG-Ala-Lys molecular complex can be obtained after dialysis purification and lyophilization. Then use conventional EDC and NHS reagents to activate the terminal carboxyl group of the mPEG-XX molecular complex to obtain mPEG-Ala-Lys-NHS.

Embodiment 3

[0041] The preparation of the activated PEG-X-Y of embodiment 3, X-Y is Val-Lys

[0042] It is synthesized by conventional amide condensation reaction, and the readily available mPEG-NHS and dipeptide (Val-Lys) are dissolved in buffers such as phosphate, HEPES or Tris-HCl at pH 7.5 at a feed ratio of 1:1. , the reaction temperature was 25° C., the mixture was stirred slowly for 60 minutes, and glycine with 5 times the molar amount of PEG was added to terminate the reaction. The mPEG-Val-Lys molecular complex can be obtained after dialysis purification and lyophilization. Then, conventional EDC and NHS reagents are used to activate the terminal carboxyl group of the mPEG-Val-Lys molecular complex to obtain mPEG-Val-Lys-NHS.

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Abstract

The invention relates to a polyethylene glycol-dipeptide-antitumour drug complex and use thereof. The invention is characterized in that cathepsin B sensitive dipeptide is adopted to couple PEG and antitumour drug, so that not only modification advantage of PEG is remained, but also specificity degradation characteristic of the cathepsin B sensitive dipeptide at tumour is fully played, and influence of PEG modification on drug activity can be overcome, thus being a better tumour therapy solution.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to polyethylene glycol-dipeptide-antitumor molecule complex and its application in tumor treatment. technical background [0002] Malignant tumors have always been a serious disease that plagues human beings, and most cancers have no cure. Chemotherapy is one of the traditional methods for the treatment of malignant solid tumors and plays an important role in clinical practice. [0003] Chemotherapeutic drugs currently used clinically have some important defects. Among them, some have poor solubility (such as paclitaxel, docetaxel). In order to solve the solubility problem, a large amount of surfactants have been added to the injection, which has brought new problems such as obvious side effects; some half-lives are too short (such as tumor necrosis factor The plasma elimination half-life of the drug is 6 minutes, and the metabolic half-life in the body is 27 minutes),...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/337A61K31/704A61K38/19A61P35/00A61K47/64
Inventor 张强王坚成戴传云
Owner PEKING UNIV
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