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Use of a mek inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors

An androgen receptor and inhibitor technology, applied in the field of medicine

Active Publication Date: 2021-09-03
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Naderi et al et al. (Naderi et al. Breast Cancer Research 2011,13:R36) found that the combination of AR antagonist Flutamide and MEK inhibitor CI-1040 or PD0325901 can be used for the treatment of ER-negative breast cancer. Regarding the relationship between AR antagonists and Other effects of MEK inhibitor combinations are rarely reported

Method used

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  • Use of a mek inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors
  • Use of a mek inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors
  • Use of a mek inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors

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Embodiment 1

[0046] Example 1. Study on the efficacy of the compound (drug A) represented by formula (II) as a single drug or in combination with the compound p-toluenesulfonate (drug B) represented by formula (I) on the castrated prostate cancer mouse model. The main observation indicators are:

[0047] Tumor volume, and relative tumor inhibition rate, TGI (%), the calculation formula is:

[0048] TGI%=(1-T / C)×100% (T and C are the relative tumor volume (RTV) or tumor weight (TW) of the treatment group and the control group at a specific time point, respectively).

[0049] In this experiment, drug A was prepared according to the method disclosed in CN103958480A; drug B was prepared according to the method disclosed in patent CN106795116A.

[0050] Cell culture: The tumor cell line VCaP was cultured in a medium DMEM (containing 10% fetal bovine serum) at 37° C. in a 5% CO 2 incubator. When the tumor cells grew to the logarithmic growth phase, the tumor cells were collected and resuspende...

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Abstract

The invention relates to the use of a MEK inhibitor combined with an androgen receptor antagonist in the preparation of a drug for treating tumors. Specifically, MEK inhibitors are selected from compounds represented by formula (I) or pharmaceutically acceptable salts thereof, and androgen receptor antagonists are selected from compounds represented by formula (II) or pharmaceutically acceptable salts thereof.

Description

technical field [0001] The invention relates to the use of MEK inhibitors combined with androgen receptor (AR) antagonists in the preparation of medicines for treating or preventing diseases mediated by androgen receptors, and belongs to the field of medicine. Background technique [0002] Prostate cancer is the second most common malignancy among men worldwide and the sixth most common cause of death. The incidence of prostate cancer in my country is lower than that in western countries, but it has been rising rapidly in recent years. According to the latest statistics from the National Cancer Center, in 2015, there were about 60,300 new cases of prostate cancer in my country, and about 26,600 deaths. [0003] The majority of prostate cancer patients in my country have characteristic androgen dependence in the growth of prostate cancer cells, so endocrine therapy that inhibits androgen action is an important means of prostate cancer treatment (Endocr Relat Cancer. June 200...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/444A61K31/4166A61P35/00A61P35/02
CPCA61K31/4166A61K31/444A61P35/00A61P35/02A61K2300/00
Inventor 杨健张曼廖成
Owner JIANGSU HENGRUI MEDICINE CO LTD
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