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Prophylactic or therapeutic agent for prostate cancer

A prostate cancer and therapeutic agent technology, applied in the field of preparations for the prevention and/or treatment of prostate cancer, can solve the problems of ignorance of the effect of cloperastine on the prevention or treatment of prostate cancer, and achieve excellent results

Pending Publication Date: 2020-12-11
KEIO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, cloperastine is not known to have a preventive or therapeutic effect on prostate cancer

Method used

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  • Prophylactic or therapeutic agent for prostate cancer
  • Prophylactic or therapeutic agent for prostate cancer
  • Prophylactic or therapeutic agent for prostate cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] 1. Screening of drug candidates for prostate cancer

[0056] For CRPC patients (n=3) who acquired resistance to cabazitaxel through CRPC therapy based on a novel AR inhibitor, the "RNeasy DSP FFPE kit" (manufactured by Qiagen) was used under the approval of the Keio University Ethics Committee. mRNA was extracted from the FFPE samples of CRPC tissues before the treatment (before the acquisition of cabazitaxel resistance) and the FFPE samples of the CRPC tissues after the treatment (after the acquisition of cabazitaxel resistance). The extracted RNA was fragmented and labeled with cDNA using "Affymetrix Gene Chip WT Terminal Labeling Kit" (manufactured by Affymetrix), washed with "Gene Chip Fluidics Station 450" (manufactured by Affymetrix), and microarray system (Gene ChipScanner 30007G (manufactured by Affymetrix Inc.), microarray analysis was performed to analyze the change rate of the gene expression profile from the CRPC cells after acquiring resistance to cabazitax...

Embodiment 2

[0058] 2. Cell proliferation inhibitory effect on prostate cancer cells

[0059] In order to confirm that cloperastine has an inhibitory effect on the cell proliferation of metastatic CRPC, the metastatic CRPC cell lines (DU145 cell line and PC3 cell line) were cultured in the presence of cloperastine, and the cell proliferation was analyzed .

[0060] [method]

[0061] After culturing the DU145 cell line and the PC3 cell line (both cells were obtained from ATCC [American Culture Collection]) on a 96-well plate for 24 hours, cloperastine hydrochloride (manufactured by Sigma-Aldrich) was added to become 0.1 μM, 1 μM or 10 μM was added to the culture solution, and after further culturing for 24 hours, the number of viable cells was measured using “Premix WST-1 Cell Proliferation Assay System” (manufactured by Takara Bio). In addition, as a control, an experiment in which the DU145 cell line and the PC3 cell line were cultured in a culture solution not containing cloperastine h...

Embodiment 3

[0066] 3. EMT inhibitory effect on metastatic CRPC

[0067] In order to confirm that cloperastine has the effect of inhibiting EMT in metastatic CRPC cells, metastatic CRPC cell lines (DU145 cell line and PC3 cell line) were cultured in the presence of cloperastine, and EMT-related factors analysis of gene expression profiles.

[0068] [method]

[0069] After the DU145 cell line and the PC3 cell line were cultured for 24 hours in the presence of 10 μM cloperastine or in the absence of cloperastine (cloperastine treatment group and control group, respectively), the "RNeasy Mini kit" was used to (manufactured by Qiagen) was used to extract mRNA. The extracted mRNA was synthesized into cDNA using "Prime Script RT reagent Kit" (manufactured by Takara Bio). In order to encode 6 factors (E-cadherin, vimentin, "zinc finger protein SNAI1", "zinc finger protein SNAI2", "zinc finger E-box binding homeobox 1", and "zinc finger E-box The mRNA expression levels of genes (CDH1 gene, VIM...

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Abstract

The present invention addresses the problem of providing a prophylactic or therapeutic agent which is for prostate cancer and which can be produced simply and inexpensively, and contains, as an activeingredient, a low molecular weight compound exhibiting antitumor effects even on intractable castration-resistant prostate cancers (particularly, castration-resistant prostate cancer having resistance to cabazitaxel, which is the most intractable prostate cancer). The prophylactic or therapeutic agent for prostate cancer (preferably, castration-resistant prostate cancer having resistance to cabazitaxel) contains cloperastine or a pharmaceutically acceptable salt thereof.

Description

technical field [0001] The present invention relates to a preparation for preventing and / or treating prostate cancer comprising cloperastine or a pharmaceutically acceptable salt thereof (hereinafter, they may be collectively referred to as "cloperastines" in some cases). Background technique [0002] Prostate cancer is a cancer that develops in the prostate, which is one of the male genitals, and is the most common cancer among men in Europe and the United States, especially in the United States. Prostate cancer is considered to be related to eating habits with a lot of animal fat intake and advanced age. In fact, in Japan, the incidence of prostate cancer has also increased rapidly in recent years along with Westernization of eating habits and aging population. For example, in 2013, prostate cancer ranked fourth bit. The prevalence of prostate cancer increases sharply after the age of 70, and it is expected to further increase in the future in developed countries such as...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4453A61P13/08A61P35/00A61P35/04
CPCA61P13/08A61K31/4453A61P35/00A61P35/04A61K31/337A61K2300/00A61K9/0053A61K45/06
Inventor 小坂威雄本乡周大家基嗣
Owner KEIO UNIV
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