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Lung cancer-targeting conjugate medicine cdGIGPQc-ScFvalphavbeta3

A drug and coupling technology, applied in the field of biomedicine, can solve the problems of large monoclonal antibody molecules, easy to produce anti-antibodies, and large side effects, and achieve the effect of fast clearance in the body, no toxic side effects, and strong targeting

Inactive Publication Date: 2017-06-06
ZHUJIANG HOSPITAL SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The new monoclonal antibody drug targeting αvβ3 has entered the clinical trial stage. However, due to the large size of the monoclonal antibody molecule, it is difficult to enter the interior of solid tumors; it is slow to clear in the body, easy to produce anti-antibodies, and has many side effects. Therefore, it is easier to develop through the capillary Vascular, small-molecule tumor suppressors capable of entering solid tumor interiors have major implications

Method used

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  • Lung cancer-targeting conjugate medicine cdGIGPQc-ScFvalphavbeta3
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  • Lung cancer-targeting conjugate medicine cdGIGPQc-ScFvalphavbeta3

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Embodiment Construction

[0029] Technical scheme of the present invention is:

[0030] (1) Design and synthesis of cdGIGPQc-ScFvαvβ3

[0031] The inventors constructed cdGIGPQc-ScFvαvβ3 by PCR method and molecular biology gene cloning technology, and preliminarily clarified its influence on the proliferation and metastasis of lung cancer cells.

[0032] (2) Targeting analysis of small molecule peptide-ScFvαvβ3

[0033] The fluorescein Alexa-labeled small molecular peptide (preliminary work has been completed) was used to construct Alexa-cdGIGPQc-ScFvαvβ3. A human nude mouse lung cancer animal model was established, and Alexa-cdGIGPQc-ScFvαvβ3 was injected into the tail vein of the mice, and the distribution in various organs of the tumor-bearing mice was dynamically observed using a fluorescence scanner to analyze its specificity.

[0034] (3) Biocompatibility and toxicity analysis of cdGIGPQc-ScFvαvβ3

[0035] ① Select SD rats and experimental dogs to observe the safety of intravenous administrati...

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Abstract

The invention discloses a lung cancer-targeting conjugate medicine cdGIGPQc-ScFvalphavbeta3. The lung cancer-targeting conjugate medicine cdGIGPQc-ScFvalphavbeta3 is prepared by coupling a small molecule peptide cdGIGPQc with a single-chain antibody ScFvalphavbeta3 of an integrin alphavbeta3. The lung cancer-targeting conjugate medicine cdGIGPQc-ScFvalphavbeta3 is a small molecule, is capable of easily penetrating through capillary vessels and can be rapidly gathered lung cancer targeting cells; the lung cancer-targeting conjugate medicine has no immunogenicity and allergic risk and has high safety, and an anti-antibody is not generated; and the lung cancer-targeting conjugate medicine can be rapidly cleared in vivo and has no toxic and side effects on the body. The cdGIGPQc-ScFvalphavbeta3 has strong targeting effect on non-small cell lung cancers, small molecule peptide can be specific bound with non-small cell lung cancer cells at any sites in vivo, the treatment effect is not limited by growth sites of tumors, and the cdGIGPQc-ScFvalphavbeta3 is especially suitable for patients suffering from distant organ metastasis type advanced lung cancers.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a coupled drug cdGIGPQc-ScFvαvβ3 targeting lung cancer. Background technique [0002] Lung cancer is one of the most common and deadly malignant tumors in the world, and its incidence rate is also the highest among all malignant tumors. At present, the main treatment mode of lung cancer is multidisciplinary comprehensive treatment, but the overall effect is not satisfactory. Molecular targeted therapy has become one of the important research topics in clinical therapy of lung cancer. [0003] Molecular targeted therapy refers to the design of corresponding therapeutic drugs aimed at the identified carcinogenic site (the site can be a protein molecule or a gene fragment of tumor cells) at the cellular molecular level. The body will specifically select the oncogenic sites to combine with each other to make the tumor cells die specifically, without affecting the normal tissu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/68A61K38/08A61P35/00
CPCA61K38/08
Inventor 张帆郭琳琅裘倩倩王琼瑶
Owner ZHUJIANG HOSPITAL SOUTHERN MEDICAL UNIV
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