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Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and histone deacetylase inhibitor and application thereof

A hepatocyte growth factor and receptor inhibitor technology, which is applied to the pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and histone deacetylase inhibitor and its application field, can solve the problem of high toxicity and patient discomfort. Tolerance and other issues

Inactive Publication Date: 2013-02-13
DINKUM INT INVESTMENT HONG KONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are many anti-tumor drugs on the market, such as alkylating agent drugs, antimetabolite drugs, anti-tumor antibiotics, immunomodulators, etc., but most of the drugs are more toxic due to large, patient intolerance

Method used

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  • Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and histone deacetylase inhibitor and application thereof
  • Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and histone deacetylase inhibitor and application thereof
  • Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and histone deacetylase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 The combination of different ratios of PF-02341066 and SAHA synergistically promotes the death of HT-29 cells, see Table 2.

[0042] Table 2

[0043]

[0044]

[0045] In the experiment investigating the death of colon cancer cell line HT-29 cells caused by related compounds, it was found that only about 20% of the cells died when 1.5μMPF-02341066 or lower concentration and 2.0μMSAHA or lower concentration were used alone; When used in combination at a lower concentration (1.0μMPF-02341066+1.5μMSAHA), a significant synergistic effect was produced, resulting in the death of about 60% of cancer cells; A more pronounced synergistic effect resulted in the death of about 90% of cancer cells.

Embodiment 2

[0046] Example 2 The combination of different ratios of PF-02341066 and SAHA synergistically promotes the death of U2-OS cells, see Table 3.

[0047] table 3

[0048]

[0049] In the experiment of investigating the death of the sarcoma cell line U2-OS cells caused by related compounds, it was found that only a small amount of cell death was observed when 1.5μMPF-02341066 or lower concentration and 1.0μMSAHA or lower concentration were used alone; When the concentration reaches 1.5μM SAHA, only about 15% of the cells die; and when the two are used together at a lower concentration (1.0μMPF-02341066+1.0μM SAHA), there is an obvious synergistic effect, resulting in the death of about 60% of the cancer cells; When the two are used together at the ratio of 1.5μMPF-02341066+1.5μM SAHA, there will be a more obvious synergistic effect, resulting in the death of about 90% of cancer cells.

Embodiment 3

[0050] Example 3 The combination of different ratios of PF-02341066 and SAHA synergistically promotes the death of D37 cells, see Table 4.

[0051] Table 4

[0052]

[0053] In the experiment of investigating the cell death of glioma cell line D37 caused by related compounds, it was found that only about 10-20% of the cells died when 2.0μMPF-02341066 or lower concentration and 1.5μMSAHA or lower concentration were used alone; When the two are combined at a lower concentration (1.5μM PF-02341066+1.0μM SAHA), there is an obvious synergistic effect, resulting in about 60% cancer cell death; when the two are combined at a ratio of 2.0μM PF-02341066+1.5μM SAHA When used, it produces a more obvious synergistic effect, resulting in the death of about 85% of cancer cells.

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Abstract

The invention relates to a pharmaceutical composition containing a hepatocyte growth factor receptor (cMet) inhibitor and a histone deacetylase (HDAC) inhibitor, and application of the pharmaceuticalcomposition in the preparation of medicaments for treating intestinal cancer, sarcoma, glioma, liver cancer, lung cancer, stomach cancer, brain tumors, pancreatic cancer, ovarian cancer, mammary cancer or prostate cancer. The pharmaceutical composition has significant synergistic effect, improves the treatment effect of the medicaments, reduces the administration dose and reduces side effects.

Description

technical field [0001] The invention relates to a pharmaceutical composition and its application in the preparation of medicines for treating cancer, in particular to a pharmaceutical composition containing hepatocyte growth factor receptor (cMet) inhibitors and histone deacetylase (HDAC) inhibitors The method and its application in the preparation of medicines for treating intestinal cancer, sarcoma, glioma, liver cancer, lung cancer, gastric cancer, brain tumor, pancreatic cancer, ovarian cancer, breast cancer or prostate cancer. Background technique [0002] The survey report of the World Health Organization shows that the global cancer situation is getting worse. In the next 20 years, the number of new patients will increase from the current 10 million to 15 million per year, and the number of deaths from cancer will also increase from 6 million to 10 million per year. Among them, colon cancer is one of the common malignant tumors, with the highest incidence rate in the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/4545A61K31/167A61K31/16A61P35/00
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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