Immune vesicle maytansine conjugate as well as preparation method and application thereof

A technology of maytansinoids and maytansinoids, applied in drug combinations, pharmaceutical formulations, nano-drugs, etc., can solve the problems of limited research, large antibody dosage, and low drug content, and achieve good biocompatibility, high efficiency and stability The effect of the package effect
CN113244175AActive Publication Date: 2021-08-13SUZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SUZHOU UNIV
Publication Date
2021-08-13

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Abstract

The invention discloses an immune vesicle maytansine conjugate as well as a preparation method and application thereof. The immune vesicle maytansine conjugate is prepared from an amphiphilic polymer, maytansine and an antibody, specifically, the functionalized amphiphilic block polymer and an amphiphilic block polymer are assembled and spontaneously cross-linked and meanwhile coupled with the maytansine through a sulfydryl-sulfur-sulfur exchange reaction, and then react with the monoclonal antibody to prepare the immune vesicle maytansine conjugate. The maytansine has broad-spectrum anti-tumor activity and is suitable for solid tumors and malignant hematological tumors, but due to the fact that maytansine is extremely high in toxicity, narrow in treatment window and incapable of being used independently, the technical scheme provides possibility for use of potent medicine DM. Experimental results show that under the high dose of the immune vesicle maytansine conjugate, mice is good in tolerance and completely survive, and the therapeutic window of the toxic molecule DM1 is effectively expanded.
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Description

technical field

[0001] The invention belongs to the technical field of polymer nano-medicines, and in particular relates to a monoclonal antibody-directed reversible cross-linked polymer vesicle maytansinoid conjugate, a preparation method thereof, and an application in tumor targeting therapy. Background technique

[0002] Maytansine (DM1) is a plant-derived hydrophobic drug with a macrocyclic lactone structure. It mainly acts on tubulin to prevent its formation in cell mitosis, thereby blocking the cell cycle and inducing apoptosis. Maytansine has been widely studied due to its excellent anti-tumor effect in preclinical experiments, but in early clinical trials, maytansine showed strong gastrointestinal toxicity and neurotoxicity, and the therapeutic window was small, so it cannot be used alone. Due to its strong toxicity, maytansine has been widely studied in recent years for the toxin warhead of antibody-drug conjugates (ADCs). At present, one Ado-transtuzumabemtansine (...

Claims

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