Application of Nifurolimus in the Preparation of Drugs for Treating Cancer-Derived Brain Metastases

A technology for nifurolimus and brain metastases, which is applied in antineoplastic drugs, drug combinations, and pharmaceutical formulas, and can solve the problems of small beneficiary population, high treatment costs, and further confirmation of the effect of intracranial tumors

Active Publication Date: 2019-12-24
柏思德天津医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its greater value may be reflected in the inhibition of peripheral primary tumors, reducing or reducing the occurrence of brain metastases; once brain metastases occur, its effect will drop sharply, and in more cases, its effect on intracranial tumors needs to be further confirmed
In addition, these emerging targeted drugs benefit a small group of people, and the cost of treatment is high. For example, the newly developed CAR-T cell therapy by Novartis has a treatment cost of up to 3 million yuan, which is out of reach for most patients

Method used

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  • Application of Nifurolimus in the Preparation of Drugs for Treating Cancer-Derived Brain Metastases
  • Application of Nifurolimus in the Preparation of Drugs for Treating Cancer-Derived Brain Metastases
  • Application of Nifurolimus in the Preparation of Drugs for Treating Cancer-Derived Brain Metastases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Determination of the Growth Inhibitory Effect of Nifurolimus on Human Tumor Cells by MTT Assay

[0041]The purpose of this experiment is to use the MTT method to measure the cell survival rate, observe the growth inhibitory effect of nifurolimus on various human tumor cells and normal cells at the cellular level, and explore whether it can inhibit the growth of tumor cells at the in vitro level , strength of action and sensitivity to different types of tumor cells, etc., providing reference information for exploring the mechanism of action of the test substance, safety evaluation, drug regimen in clinical trials, and selection of tumor types.

[0042] Cell lines: human bone marrow neuroblastoma SH-SY5Y, human neuroblastoma human neuroblastoma SK-N-SH, human glioma cells Hs683, human glioma cells U251, human brain astrocytes Plasmoblastic tumor U87MG, human brain tumor cell SF126, human non-small cell lung cancer cell H460, human liver cancer cell Bel7402, human breast c...

Embodiment 2

[0052] Therapeutic effect of nifurolimus on H460 brain metastases from human lung cancer in nu / nu nude mice

[0053] Experimental purpose To evaluate the therapeutic effect of different concentrations of Nifurtimox on nu / nu nude mice bearing human lung cancer brain metastases H460.

[0054] Experimental material Tumor cell line: human lung cancer H460 cell line.

[0055] Experimental animals: adult Nu / Nu nude mice (Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.), 18-20 g, female. The experimental animals were housed in sterile IVC cages with independent ventilation, 5 per cage. Litter is 60 Co radiation sterilized corncob litter, particle size 4-6mm. Rats were fed with sterilized feed specially formulated for mice, and purified water was freely available to drink. The temperature in the animal laboratory is kept at about 25°C, the relative humidity is kept at 40-70%, and the light is 12 hours a day.

[0056] Experimental scheme: Culture cells, infect H460 ...

Embodiment 3

[0063] Inhibitory effect of nifurolimus on growth of human breast cancer cell line MCF-7 metastatic tumor in nude mice brain

[0064] Experimental purpose This experiment selects human breast cancer cell line MCF-7 to establish a nude mouse model of brain metastases, observes the inhibitory effect of nifurolimus on its growth, and provides reference for clinical application.

[0065] Experimental Materials

[0066] testing sample

[0067] Name: Nifurtimox (English name: Nifurtimox).

[0068] experiment system

[0069] 1. Strain: Nu / Nu nude mice (Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.).

[0070] 2. Tumor strain: human breast cancer cell MCF-7.

[0071] Tumor model construction and detection methods

[0072] Experimental Design Basis: Adoption Standards: Experimental design is carried out in accordance with "Guiding Principles for Non-clinical Research Techniques of Cytotoxic Antineoplastic Drugs".

[0073] Establishment of intracranial xenograft tu...

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Abstract

The invention provides an application of nifurtimox in the preparation of drugs for treating cancer-derived metastatic encephaloma. The cancer preferably refers tois lung cancer, breast cancer or skincancer. The nifurtimox is an anti-parasitic drug. The metastatic encephaloma of the cancer is a tumor formed by the metastasizing of malignant tumors from other parts of the body to the intracalvarium, and the tumor is serious in consequences and high in a mortality rate. However, few drugs are available for the treatment of metastatic encephaloma, so the invention provides the application of nifurtimox in the preparation of drugs for treating cancer-derived metastatic encephaloma, which greatly solves this technical problem.

Description

technical field [0001] The invention relates to the application of nifurolimus in the preparation of medicines for treating brain metastases derived from cancer, and belongs to the field of medicines. [0002] technical background [0003] Metastatic brain tumors are often the most common feature of cancer, especially lung, breast, or skin cancer. [0004] The proportion of melanoma with brain metastases reaches 40%. Brain metastases are the leading cause of death in patients with advanced non-small cell lung cancer (NSCLC) and breast cancer. Current drug options for treating such patients are limited, especially after brain metastases. [0005] Primary lung cancer is one of the most common malignant tumors in my country, and one of the most common distant metastatic sites of lung cancer is the brain. Among all brain metastases, lung cancer ranks first in men, followed by malignant melanoma; in women, lung cancer ranks first, followed by breast cancer. Brain is one of the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/541A61P35/04A61P35/02
CPCA61K31/541A61P35/02A61P35/04
Inventor 吴文涛任弘光
Owner 柏思德天津医药科技有限公司
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