Targeted medicament for curing prostate diseases

A technology for prostate and prostate cancer, applied in drug combination, urinary system diseases, anti-tumor drugs, etc., can solve problems such as unsatisfactory treatment of prostate diseases, toxic side effects, and adverse effects on patients

Active Publication Date: 2012-08-22
上海市生物医药技术研究院 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the lack of targeting when administering these small molecule drugs often requires the use of higher doses to achieve the concentrations required for therapeutic effects in prostate tissue
However, large doses of drugs are often accompanied by some toxic side effects, which have adverse effects on patients
Therefore, the treatment of prostate disease is still unsatisfactory

Method used

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  • Targeted medicament for curing prostate diseases
  • Targeted medicament for curing prostate diseases
  • Targeted medicament for curing prostate diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Preparation of Epuletide-PSA Antibody by DCC Method (Method 1)

[0103] EDC (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) is a water-soluble carbodiimide used as an activating reagent for carboxyl groups in amide synthesis . The ratio of Epulet to EDC is 1M:1.2-1.8M. The pH range of the activation reaction is 4.0-6.0. After the activation reaction, the PSA antibody (the antibody is a mouse monoclonal antibody) was added, and the ratio of the amount of the PSA antibody added to apretide was 1M:10-100M. The DEAE ion exchange column is used for chromatographic separation, that is, the E-PSA conjugate is suspended in a buffer solution, and the buffer solution uses 100mM Tris, pH8.6, to remove small molecular compounds and obtain a purified conjugate product.

Embodiment 2

[0105] Preparation of Aprelate-PSA Antibody by DCC Method (Method 2)

[0106] EDC (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride) is a water-soluble carbodiimide used as an activating reagent for carboxyl groups in amide synthesis . The ratio of Epulet to EDC is 1M:1.2-1.8M. The pH range of the activation reaction is 4.0-6.0. After the activation reaction is completed, add PSA antibody, the ratio of the amount of PSA antibody added to eprelate is 1M:10-100M, and a small amount of N-hydroxysuccinimide (NHS) is added at the same time to complete the coupling reaction. The DEAE ion exchange column is used for chromatographic separation, that is, the E-PSA conjugate is suspended in a buffer solution, and the buffer solution uses 100mM Tris, pH8.6, to remove small molecular compounds and obtain a purified conjugate product.

Embodiment 3

[0108] Preparation of Epuletide-PSA Antibody by DCC Method (Method 3)

[0109] Add cyanogen bromide to Apretide for activation (the weight ratio to cyanogen bromide is 1:0.5), and then add adipic hydrazide for treatment, the derivatization rate is 1-3%. After the activation reaction finishes, add PSA antibody and carbodiimide (19.17mg / ml), the ratio of the amount that PSA antibody adds and aprelate is 1M: 10-100M, adds a small amount of N-hydroxyl succinimide ( NHS), together to complete the coupling reaction. The DEAE ion exchange column is used for chromatographic separation, that is, the E-PSA conjugate is suspended in a buffer solution, and the buffer solution uses 100mM Tris, pH8.6, to remove small molecular compounds and obtain a purified conjugate product.

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Abstract

The invention provides a targeted medicament for curing prostate diseases. Particularly, the invention provides a targeted curative molecule with a structure shown as 'T-A'. In a formula, T is a targeted moiety aiming at prostate cells; A is a compound having curative activity on the prostate diseases; and T and A are bonded through a chemical bond or a covalent bond. The targeted medicament provided by the invention maintains targeting property of the conventional prostate specific antigen (PSA) antibody and basically maintains all the activity of small molecule compounds. Compared with the conventional single Epristeride and Finasteride, the dosage of the targeted medicament provided by the invention is greatly reduced by about 1,000 times, so that toxic and side effect generated in theusing process of the medicament is reduced.

Description

technical field [0001] The present invention relates to the fields of medicine and therapy. Specifically, it relates to a targeted drug comprising a targeting moiety and a molecule for treating prostate diseases. The invention also relates to a pharmaceutical composition containing the targeted drug, and discloses a method for treating prostate diseases, especially the use of the targeted drug in the treatment of prostate cancer. Background technique [0002] Among male diseases, the incidence of prostate disease is increasing. Prostate diseases are mainly composed of three diseases: prostatitis, benign prostatic hyperplasia and prostate cancer. The latter two are more difficult to treat, especially prostate cancer will cause some patients to die. [0003] Prostate cancer is one of the most common cancers that afflict men over 65 years of age. Prostate cancer is believed to affect approximately one million American men in the United States. Although less than 3 percent ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/56A61P13/08A61P35/00A61K47/68
Inventor 孙祖越黄文华
Owner 上海市生物医药技术研究院
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