Medicament for treating tumor with csf1r as drug target and preparation method thereof

A technology of drugs and oils, which is applied in the field of drugs for treating tumors and its preparation, can solve the problems of high recurrence rate, inability to remove the cause of disease, uncertain cause of disease, etc., and achieve the effect of improving prognosis

Active Publication Date: 2022-02-11
THE FIRST AFFILIATED HOSPITAL ZHEJIANG UNIV COLLEGE OF MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The existing treatment of Langerhans cell tumor needs to choose different treatment options according to the different conditions, but because the cause of the disease is uncertain, the cause cannot be fundamentally eliminated, so the recurrence rate is high

Method used

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  • Medicament for treating tumor with csf1r as drug target and preparation method thereof
  • Medicament for treating tumor with csf1r as drug target and preparation method thereof
  • Medicament for treating tumor with csf1r as drug target and preparation method thereof

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preparation example Construction

[0037] In order to solve the above technical problems, the present invention provides an application of CSF1R: as a therapeutic target of Langerhans cell tumor or tumor-associated macrophages, to prepare a medicament and a preparation method.

[0038] The present invention provides the application of CSF1R as a drug target in the treatment of Langerhans cell tumors or tumor-associated macrophages. The CSF1R is a transmembrane receptor of tyrosine kinase and CSF1 / Member of the PDGF receptor family.

[0039] The specific protein sequence of CSF1R in Rattus norvegicus is:

[0040]

[0041]

[0042] The specific protein sequence of CSF1R in humans is:

[0043]

[0044] The present invention provides a medicament for treating Langerhans cell tumor or tumor-associated macrophages with CSF1R as a drug target, that is, oral oil preparation of Ki20227 is used to antagonize CSF1R. Ki 20227 acts as an antagonist of CSF1R.

[0045] The molecular mass of Ki 20227 is 480.54, an...

example 1

[0051] Example 1: The present invention provides a new target for the treatment of Langerhans cell tumor - CSF1R. Specifically, mice were treated with CSF1R antagonist Ki 20227 oral oil and CSF1R inhibitory monoclonal antibody vehicle (eg figure 2 ), Langerhans cells (CD45+CD11b+epCAM+) were screened out by flow cytometry (such as image 3 ), the proportion of Langerhans cells was compared with that of the control group, and the proportion of Langerhans cells in the two groups of mice treated with Ki 20227 and CSF1R inhibitory monoclonal antibody were significantly reduced (such as Figure 4 A, 4B).

[0052] Further, the immunofluorescence technique was used to verify that the Langerhans cells in the mouse skin were significantly reduced after treatment with Ki 20227 and CSF1R inhibitory monoclonal antibody compared with those before treatment (such as Figure 5 ).

[0053] The two medicaments for targeting and inhibiting Langerhans cell tumors provided by the present inve...

Embodiment approach

[0055] Implementation method: Dissolve 0.5g Ki 20227 in 5ml 50% DMSO, add to 30ml monooleate after dissolving, heat to 40°C, mix well, add 65ml oleic acid, mix well, and then make 5mg / ml Ki 20227 oral oil formulation.

[0056] 2. A method for preparing a CSF1R inhibitory monoclonal antibody solvent.

[0057] Implementation method: Add 1 mg of anti-mouse CSF1R (CD115) with the clone number AFS98 into 2 ml of PBS containing 0.1% BSA at 4°C, mix thoroughly to obtain a 500 μg / ml CSF1R inhibitory monoclonal antibody solvent, and store at 4°C.

[0058] CSF1R antagonist Ki 20227 oral oil and CSF1R inhibitory monoclonal antibody solution can reduce Langerhans cells in Langerhans cell tumors.

[0059] 1. Flow cytometry analysis of the effects of Ki 20227 oral oil preparation and CSF1R inhibitory monoclonal antibody solution on mouse Langerhans cells.

[0060] Implementation method: Treat mice with CSF1R antagonist Ki 20227 oral oil and CSF1R inhibitory monoclonal antibody solution re...

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Abstract

The invention belongs to the field of biomedicine, and mainly relates to a medicament for treating tumors using CSF1R as a drug target and a preparation method thereof. The invention relates to a new treatment site for Langerhans cell tumors or tumor-associated macrophages, in particular to Targeting CSF1R to treat Langerhans cell tumors or tumor-associated macrophages, Ki 20227 oral oil formulation targeting CSF1R and CSF1R inhibitory monoclonal antibody solvent, including using them to prepare drugs as targeted therapy Langerhans Stein cell tumor or tumor-associated macrophages. CSF1R drug target and its antagonist Ki 20227 oral oil preparation and CSF1R inhibitory monoclonal antibody solution have great clinical application value in the preparation of drugs for treating Langerhans cell tumor or inhibiting tumor-associated macrophages to treat malignant tumors The invention provides a new method, medicine and preparation method for treating Langerhans cell tumor or suppressing tumor-associated macrophages to treat malignant tumors.

Description

technical field [0001] The invention belongs to the field of biomedicine, and mainly relates to a medicament for treating tumors with CSF1R as a drug target and a preparation method thereof. Background technique [0002] Malignant tumors are diseases that seriously endanger human life and health. In my country, about 3.804 million people suffer from cancer every year, and about 2.296 million people die from cancer every year. According to the 2012 World Cancer Report of the World Health Organization, there were 3.804 million newly diagnosed cancer cases in China, accounting for 21.8% of the global total; while the annual death toll was 2.296 million, accounting for 24.0% of the global annual cancer death toll. What's more serious is that these data are increasing year by year at an alarming rate. Therefore, it is of great significance to human health to explore the molecular mechanism of cancer and find its effective treatment. [0003] Tumor-associated macrophages (TAMs) ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/4709A61K39/395A61K9/08A61K47/14A61K47/42A61P35/00
CPCA61K45/00A61K31/4709A61K9/0053A61K9/08A61K47/14A61K47/42A61P35/00C07K16/2866A61K2039/505
Inventor 盛剑鹏张俊磊白雪莉梁廷波
Owner THE FIRST AFFILIATED HOSPITAL ZHEJIANG UNIV COLLEGE OF MEDICINE
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