Multi-drug-loading-point and high-drug-loading ligand-drug conjugate

A technology of drug conjugates and ligands, applied in the field of medicine, can solve the problems of unfavorable improvement of the drug loading capacity of the conjugates and few drug loading points, etc.

Active Publication Date: 2018-10-16
JENKEM TECH CO LTD (LIAONING)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Patent document CN201510160703.5 discloses an antibody-conjugated drug, which is obtained by covalently coupling drug molecules and Fab fragments with heterobifunctional polyethylene glycol, although the drug-loading point of the above-mentioned antibody conjugate is determined , The drug-loading ratio is clear, but there are fewer drug-loading points, which is not conducive to improving the drug-loading capacity of the entire conjugate

Method used

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  • Multi-drug-loading-point and high-drug-loading ligand-drug conjugate
  • Multi-drug-loading-point and high-drug-loading ligand-drug conjugate
  • Multi-drug-loading-point and high-drug-loading ligand-drug conjugate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0193] Example 1: Synthesis of four-arm polyethylene glycol maleimide-monoacetate succinimidyl ester (V-3)

[0194]

[0195] step:

[0196] The four-arm polyethylene glycol maleimide-monoacetate succinimide ester (V-3) was prepared by referring to the steps of Examples 1-9 in the patent application CN201610398765.4.

[0197] NMR(DMSO)δ: 2.32(t,6H, ), 2.82(s, 4H, ),3.15(q,6H,CH 2 CH 2 NH), 4.60(s,2H,CH 2 COO), 6.99(s,6H, ).

[0198] [PEG-2] Synthesis Example

Embodiment 2

[0199] Example 2: SH-PEG-(CONHI) 3 (5K)(T2-4) Preparation

[0200] HS-PEG-(CONHI) 3

[0201] T2-4

Embodiment 3

[0203] Example 3: Preparation of SH-PEG-CONHI (3.5K) (T5-6)

[0204] HS-PEG-CONHI

[0205] T5-6

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Abstract

The invention discloses a multi-drug-loading-point and high-drug-loading ligand-drug conjugate. The ligand-drug conjugate has a structure shown in general formula I, and has the characteristics of high loading capacity, high drug efficacy, low toxicity, and low risks. The ligand-drug conjugate can be particularly used for connecting a low toxicity drug molecule, thereby extending a therapeutic window. Furthermore, an antibody-conjugated drug molecule provided by the invention has the characteristics of multiple drug-loading points and high drug-loading capacity, and thus an antibody-conjugateddrug can carry a large amount of low toxicity drug molecules and achieve a therapeutic effect without depending on antibody targeting or high toxicity drugs. TM-{R<2>-PEG<1>-[R<1>-PEG<2>-(R<3>-A'-D)<n>]<m>}l(I).

Description

Technical field [0001] The present invention relates to the technical field of medicine, in particular to a drug conjugate with multiple drug loading points, high drug loading base and a drug composition, and a preparation method and application thereof. Background technique [0002] Antibody-Drug Conjugates (ADC) are the coupling products of monoclonal antibodies (Monoclonal Antibody, mAb) with biologically active small molecule drugs through linkers. Antibody-drug conjugates can specifically recognize the characteristics of tumor cells. "Precisely" deliver small molecule drugs to tumor cells, increase the concentration of the drug at the tumor site while reducing the concentration of the drug in normal tissues and organs, achieving a highly effective and low-toxic anti-tumor effect. The US FDA approved the first antibody-conjugated drug gemtuzumab ozogamicin in 2000 Although the drug was withdrawn from the market after 10 years due to safety risks and other reasons, the US FDA...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/68A61K47/60A61K47/65A61P35/00A61P37/02A61P31/18A61P31/04A61P31/16A61P31/22A61P31/14A61P31/20A61P31/12A61P33/06A61P33/02
CPCA61K47/60A61K47/65A61P31/04A61P31/12A61P31/14A61P31/16A61P31/18A61P31/20A61P31/22A61P33/02A61P33/06A61P35/00A61P37/02A61K31/436A61K47/6855A61K47/6883A61K47/6803Y02A50/30
Inventor 宋艳萍杜景辉王雷敏汪进良林美娜冯泽旺赵宣
Owner JENKEM TECH CO LTD (LIAONING)
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