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Application of EZH2 inhibitor in preparation of drugs for treatment of non-small cell lung cancer

A non-small cell lung cancer and inhibitor technology, applied in the field of EGFR-TKIs non-small cell lung cancer treatment, can solve the problems of insensitivity, disease treatment failure, drug resistance, etc., to inhibit proliferation, inhibit migration and proliferation, and reduce drug resistance sexual effect

Pending Publication Date: 2019-08-16
GENERAL HOSPITAL OF TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For NSCLC patients with advanced EGFR mutations, the first-line treatment with first-generation EGFR-TKI drugs is significantly better than platinum-based chemotherapy in terms of efficiency and PFS, but the application of first-generation EGFR-TKI therapy will face a serious problem : The vast majority of lung cancer patients will develop drug resistance to varying degrees about 1 year after treatment, leading to disease recurrence and treatment failure, which is called acquired drug resistance; at the same time, some lung cancer patients are not sensitive to EGFR-TKI, primary resistance

Method used

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  • Application of EZH2 inhibitor in preparation of drugs for treatment of non-small cell lung cancer
  • Application of EZH2 inhibitor in preparation of drugs for treatment of non-small cell lung cancer
  • Application of EZH2 inhibitor in preparation of drugs for treatment of non-small cell lung cancer

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Experimental program
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Effect test

Embodiment 1

[0064] The embodiment of the present invention discloses the application of an EZH2 inhibitor in the preparation of a drug for treating non-small cell lung cancer. The EZH2 inhibitor is GSK343, and the inhibitor GSK343 ​​and gefitinib are administered simultaneously.

Embodiment 2

[0066] The embodiment of the present invention discloses the application of an EZH2 inhibitor in the preparation of a drug for treating non-small cell lung cancer. The EZH2 inhibitor is DZNep, and the inhibitor DZNep is compounded with gefitinib.

Embodiment 3

[0067] Example 3 Verifies the effect of the administration mode of Example 1 on the sensitivity of acquired drug-resistant PC9 / AB2 cells and primary drug-resistant A549 and H1299 cells to gefitinib

[0068] Step 1. Preparation of gefitinib-acquired drug-resistant cell line: Long-term exposure of gefitinib-sensitive cell line PC9 cells to gefitinib to establish a gefitinib-resistant cell line PC9 / AB2. During the process, 10μM / L gefitinib was continuously added to RPMI-1640 medium to maintain its drug resistance. Among them, PC9 cells were purchased from Cybertron (Shanghai) Biotechnology Co., Ltd., and PC9 cells and PC9 / AB2 cells were preserved by Tianjin Lung Cancer Research Institute, General Hospital of Tianjin Medical University. At the same time, we selected A549 and H1299 (both cells are EGFR wild-type cells) cell lines as the primary resistance model of gefitinib. Both cells were purchased from the ATCC cell bank in the United States.

[0069] Step 2. Four kinds of cells wer...

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Abstract

The invention discloses an application of an EZH2 inhibitor in preparation of drugs for treatment of non-small cell lung cancer. The EZH2 inhibitor is GSK343 and DZNep, the inhibitor GSK343 or DZNep can be compounded with the first-generation EGFR-TKI drugs, respectively, the drug resistance of non-small cell lung cancer can be effectively reduced, the migration and proliferation of cancer cells are inhibited, and application provides a novel treatment idea for the treatment of lung cancer, which has brought good news to the patients.

Description

Technical field [0001] The present invention relates to the technical field of EGFR-TKIs non-small cell lung cancer treatment, more specifically to the application of EZH2 inhibitor GSK343 ​​or DZNep in the preparation of drugs for the treatment of non-small cell lung cancer. Background technique [0002] Lung cancer is one of the most common malignant tumors in my country, with a high incidence and fatality rate, and the incidence rate is increasing year by year, ranking first among various malignant tumors in some large and medium cities in my country. Among them, non-small cell lung cancer (NSCLC) accounts for 80% of all lung cancers. The treatment of early lung cancer is mainly based on surgery, but due to the lack of obvious early symptoms and other reasons, 30%-40% of patients have missed the best period of surgery at the time of diagnosis, and there is also a higher recurrence rate and metastasis rate after lung cancer surgery. . For patients who have missed the indicati...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K31/437A61K45/06A61K31/5377A61P11/00A61P35/00
CPCA61K31/437A61K31/496A61K31/5377A61K45/06A61P11/00A61P35/00A61K2300/00
Inventor 陈军刘红雨宫颢李永文张洪兵李颖袁茵施睿峰李伟婷
Owner GENERAL HOSPITAL OF TIANJIN MEDICAL UNIV
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