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CpG medicine and anthracene ring medicine compound, preparation method and application

A drug compound and anthracycline technology, applied in the field of biomedicine, can solve the problems of reducing immune activation of CpG drugs, congestive heart failure, unfavorable immunotherapy, etc., to prevent tumor immune escape, reduce toxic side effects, improve Immunogenic effects

Pending Publication Date: 2021-06-29
NANJING LUYE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, higher levels of anthracyclines have dose-dependent cardiotoxicity, manifested as various arrhythmias, and myocardial necrosis or even congestive heart failure when the cumulative dose is large
Moreover, the cytotoxicity of anthracyclines is non-specific, it can not only kill tumor cells but also immune cells and normal cells, so a high proportion of anthracyclines will reduce the immune activation effect of CpG drugs, Not conducive to immunotherapy

Method used

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  • CpG medicine and anthracene ring medicine compound, preparation method and application
  • CpG medicine and anthracene ring medicine compound, preparation method and application
  • CpG medicine and anthracene ring medicine compound, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: take by weighing 5mg pirarubicin (Dao Zhongdao (Heze) Pharmaceutical Co., Ltd.), be mixed with the pirarubicin stock solution of 2mg / mL with distilled water; Take by weighing 5mg CpG-1 (sequence: 5'-tcgaacgttcgaacgttcgaacgttcgaat -3' (full thiophosphorylation modification of phosphodiester bonds), manufacturer: Guangzhou Ruibo Biotechnology Co., Ltd.) was prepared into 1 mg / mL CpG-1 stock solution with HEPES buffer. Mix 2 mL of CpG-1 stock solution with 0.2 mL of pirarubicin stock solution, and stir at room temperature for 5 min to obtain the complex of CpG-1 and pirarubicin.

Embodiment 2

[0039] Embodiment 2: Weigh 5mg epirubicin (Dao Zhongdao (Heze) Pharmaceutical Co., Ltd.), and prepare 2mg / mL epirubicin stock solution with distilled water; Weigh 5mg CpG-2 (sequence: 5'-gGGGTCGTCGACGAggggG -3' (lowercase letters represent phosphodiester bond modified by phosphorothioation), manufacturer: Guangzhou Ruibo Biotechnology Co., Ltd.) was prepared into 1 mg / mL CpG-2 stock solution with HEPES buffer. Mix 2 mL of CpG-2 stock solution with 0.1 mL of epirubicin stock solution, and stir at room temperature for 2 h to obtain the complex of CpG-2 and epirubicin.

Embodiment 3

[0040] Embodiment 3: Weigh 5mg doxorubicin (hydrochloride form, Daozhongdao (Heze) Pharmaceutical Co., Ltd.), and prepare the doxorubicin stock solution of 2mg / mL with distilled water; Weigh 5mg CpG-2 (sequence : 5'-gGGGTCGTCGACGAggggG-3' (lowercase letters represent phosphodiester bonds modified by phosphorothioation), manufacturer: Guangzhou Ruibo Biotechnology Co., Ltd.) Prepare 1mg / mL CpG-2 stock solution with HEPES buffer . Mix 2 mL of CpG-2 stock solution with 0.33 mL of doxorubicin stock solution, and stir at room temperature for 1.5 h to obtain the CpG-2 and doxorubicin complex.

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Abstract

The invention discloses a CpG medicine and anthracene ring medicine compound, which belongs to the field of cancer immunotherapy. A mass ratio of a CpG medicine to an anthracene ring medicine is 3:1-20:1, the anthracene ring medicine at a low dosage can assist the CpG medicine in realizing more effective tumor immunotherapy, and in addition, the toxic or side effect of the anthracene ring medicine can be lowered. The invention also comprises individual utilization of the CpG medicine and anthracene ring medicine compound or combined utilization of the CpG medicine and anthracene ring medicine compound and other medicines, or a pharmaceutical acceptable carrier is added to prepare any clinically acceptable dosage. The invention specifically provides a preparation method and a purpose of the CpG medicine and anthracene ring medicine compound.

Description

technical field [0001] In the field of biomedical technology, it specifically relates to a compound, preparation method and application of CpG drugs and anthracycline drugs. Background technique [0002] Malignant tumor is a common disease that seriously endangers human life and health, and has become a major cause of death in the world. Since the occurrence of cancer is a gradual accumulation process, the morbidity and mortality show an exponential upward trend with age. With the development of the national economy, the progress of medical care and the extension of life expectancy in China, the population distribution has entered the aging stage, and the age distribution of the main population is still increasing year by year, the aging is becoming more and more serious, and the environmental pollution is still serious. Tumor has become the number one killer of disease death in our country. [0003] At present, the means of clinical treatment of cancer are mainly surgery,...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/7088A61K31/704A61K31/722A61K31/7048A61K31/136A61P35/00A61P31/00
CPCA61K45/06A61K31/7088A61K31/704A61K31/722A61K31/7048A61K31/136A61P35/00A61P31/00A61K2300/00
Inventor 张国喜田烽椿程昕伟徐凯陈文忠
Owner NANJING LUYE PHARMA
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