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Liposome composition of compound with STING agonistic activity, preparation method and application of liposome composition

A technology of liposomes and compounds, applied in the directions of drug combination, liposome delivery, organic active ingredients, etc., can solve the problems of limited clinical application, high safety risk, tumor growth and metastasis inhibition, etc.

Pending Publication Date: 2022-02-18
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Although preclinical results show that STING agonists are directly injected into tumors (including a variety of refractory and metastatic solid tumors) and tumors disappear, and tumor growth and metastasis in other parts are also significantly inhibited, but their clinical application is still limited
This is mainly due to the limitation of indications, difficult operation and high safety risk of the route of intratumoral injection. Therefore, the optimization of the route of administration of this type of compound is still a hot and difficult point in current research. Development is of great significance to improve patient compliance, reduce clinical risk, expand the scope of indications and improve therapeutic effect

Method used

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  • Liposome composition of compound with STING agonistic activity, preparation method and application of liposome composition
  • Liposome composition of compound with STING agonistic activity, preparation method and application of liposome composition
  • Liposome composition of compound with STING agonistic activity, preparation method and application of liposome composition

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[0037] definition

[0038] In the present invention, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art. Meanwhile, in order to better understand the present invention, definitions and explanations of related terms are provided below.

[0039] As used herein, the term "liposome" refers to a self-assembled structure comprising one or more amphiphilic lipid bilayers, each lipid bilayer comprising two oppositely oriented amphiphilic lipid monolayer. Amphipathic lipids comprise a polar (hydrophilic) head group covalently linked to one or two or more nonpolar (hydrophobic) acyl or alkyl chains. The very unfavorable contacts between the hydrophobic acyl chains and the surrounding aqueous medium cause the amphiphilic lipid molecules to align themselves so that the polar headgroups are oriented towards the surface of the bilayer and the acyl chains are oriented towards the interior of the bila...

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Abstract

The invention relates to a liposome composition of a compound with STING agonistic activity, a preparation method and application of the liposome composition. Specifically, the invention relates to a liposome of a compound as shown in a formula I. The liposome contains a liposome membrane and an inner water phase encapsulated in the liposome membrane, wherein the inner water phase contains a compound formed by metal ions and the ionized compound as shown in the formula I. The liposome can improve the tissue targeting property of the compound shown in the formula I, enhance the anti-tumor curative effect, prolong the blood circulation time, enhance the compliance of a patient and / or reduce the clinical medication risk;.

Description

technical field [0001] The present invention relates to the field of preparations, in particular to a liposome composition of a compound (especially compound A) with STING agonistic activity and its preparation method and application. Background technique [0002] Stimulator of interferon genes (STING) is a protein encoded by the TMEM173 gene, which contains a total of 379 amino acids. STING targets the endoplasmic reticulum through its N-terminal region, and the C-terminal contains an action / activation region, which can be activated by 2'3'-cGAMP or DNA receptors in the cytoplasm, and is a key factor in mediating innate immune signal transduction one. STING is highly expressed in immune cells. Once activated, STING receptors will initiate a cascade of innate immune responses through various pathways, including stimulating immune cells to secrete various cytokines, and then induce adaptive immune responses. Studies have found that STING activation mainly leads to the activ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/381A61K9/127A61P35/00
CPCA61K47/6911A61K31/381A61P35/00A61K9/1278
Inventor 张瑞霞苏正兴郝斐刘厦李明赵栋王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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