A targeting ligand-drug conjugate with endocytosis-mediated function

A technology of targeting ligands and conjugates, applied in the field of biomedical chemistry, can solve the problems of animal poisoning death, low efficacy, high toxicity, etc., and achieve the effects of enhancing drug efficacy, reducing drug toxicity, and ensuring stability.

Active Publication Date: 2021-05-04
COHERENT BIOPHARMA (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, when they are coupled with conventional chemotherapeutic drugs (such as doxorubicin, paclitaxel), the curative effect is low, and after coupling with high-efficiency drug molecules (such as MMAE, DM1, etc.), which are commonly used in ADCs, the toxicity is high, and the effective dose for tumor treatment will lead to animal poisoning death

Method used

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  • A targeting ligand-drug conjugate with endocytosis-mediated function
  • A targeting ligand-drug conjugate with endocytosis-mediated function
  • A targeting ligand-drug conjugate with endocytosis-mediated function

Examples

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Embodiment Construction

[0027] The preparation method of the present invention is specifically described below in conjunction with the examples:

[0028] The present invention discloses a targeting ligand-drug conjugate with cell endocytosis mediating function. The drug conjugate includes a drug molecule and a linker coupled to the drug molecule. The drug conjugate The body also includes molecules with endocytosis mediation and ligands that specifically bind to cell surface receptors. The ligands can be polypeptides or small molecule ligands, but there are also some special ligands that also have endocytosis. Function and target receptor binding function (such as folic acid, P11, P12 polypeptides). The endocytosis mediating molecule and the ligand can be coupled with each other, then coupled with a drug molecule or a linker to form a drug conjugate, or separately coupled with one of the drug molecule and the linker to form a drug conjugate.

[0029] Wherein, the molecule with endocytosis mediating e...

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Abstract

The present invention discloses a targeting ligand-drug conjugate with cell endocytosis mediating function, the drug conjugate includes a drug molecule and a linker coupled with the drug molecule, characterized in that the The drug conjugates also include molecules with a mediating effect and ligands that specifically bind to cell surface receptors, the ligands are polypeptides or small molecule ligands, and the molecules and ligands can be coupled to each other, and It is coupled with a drug molecule or a linker to form a drug conjugate, or is separately coupled with one of the drug molecule and the linker to form a drug conjugate. The beneficial effects of the present invention are mainly reflected in: the combination of targeting and endocytic (membrane-penetrating) structures, so that any ligand-targeting polypeptide can be used as a guiding part, thereby broadening the targeting range of such drugs. The conjugate ensures the stability of the drug in circulation in the body and reduces the toxicity of the drug.

Description

technical field [0001] The invention relates to a drug conjugate, in particular to a targeting ligand-drug conjugate with a cell endocytosis mediating function, and belongs to the field of biomedical chemistry. Background technique [0002] Usually, the pathological and physiological characteristics of diseased cells are significantly different from those of normal cells, one of which is the specific or overexpressed substances (such as: antigens, chemical signals, receptors, etc.) on the surface of diseased cells. No expression or low expression. Antibody-drug conjugates (ADCs) and polypeptide-drug conjugates (PDCs) treat diseases based on this principle. Although some drugs have been marketed or entered clinical research, due to the principle of drug design, ADC and PDC drugs have great limitations in clinical application. [0003] ADC is currently mainly used in the field of tumor therapy. The targeting antibody used has a very high affinity for tumor cell surface anti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K31/537A61P35/00A61P35/02A61P37/02A61P9/00
Inventor 黄保华戴建王中波谢雪原刘小栋胡新礼
Owner COHERENT BIOPHARMA (SUZHOU) LTD
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