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Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and mitogen extracellular kinase inhibitor and application thereof

A technology of hepatocyte growth factor and receptor inhibitor, which is applied to the pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and mitogen extracellular kinase inhibitor and the field of use thereof, can solve the problem of patient intolerance, Toxicity, etc.

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 mitogen extracellular kinase inhibitor and application thereof
  • Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and mitogen extracellular kinase inhibitor and application thereof
  • Pharmaceutical composition containing hepatocyte growth factor receptor inhibitor and mitogen extracellular kinase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 The combination of different ratios of PF-02341066 and ARRY-142886 synergistically promotes the death of HepG2 cells, see Table 2.

[0044] Table 2

[0045]

[0046] In the experiment investigating the cell death of liver cancer cell line HepG2 caused by related compounds, it was found that when 2.0 μM PF-02341066 or lower concentration and 0.25 μM ARRY-142886 or lower concentration were used alone, there was only a small amount of cell death; When the drug concentration reaches 0.5μM ARRY-142886, only about 20% of the cells die; and when the two are combined at a lower concentration (1.0μM PF-02341066+0.25μM ARRY-142886), there is an obvious synergistic effect, resulting in About 60% of the cancer cells died; when the two were combined at the ratio of 2.0μMPF-02341066+0.5μMARRY-142886, there was a more obvious synergistic effect, resulting in the death of about 100% of the cancer cells.

Embodiment 2

[0047] Example 2 The combinations of PF-02341066 and ARRY-142886 in different ratios synergistically promote the death of AsPC-1 cells, see Table 3.

[0048] table 3

[0049]

[0050] In the experiment of examining the cell death of pancreatic cancer cell line AsPC-1 caused by related compounds, it was found that when 1.5 μM PF-02341066 or lower concentration and 0.5 μM ARRY-142886 or lower concentration were used alone, there was only a small amount of cell death; even When the concentration of single drug was increased to 2.0μM PF-02341066 or 1.0μM ARRY-142886, only about 15-20% of the cells died; There is an obvious synergistic effect, resulting in the death of about 60% of cancer cells; when the two are combined at a ratio of 2.0μMPF-02341066+1.0μMARRY-142886, a more obvious synergistic effect is produced, resulting in the death of about 90% of cancer cells.

Embodiment 3

[0051] Example 3 The combination of PF-02341066 and ARRY-142886 in different ratios synergistically promotes the death of Hs766T cells, see Table 4.

[0052] Table 4

[0053]

[0054] In the experiment of investigating the death of pancreatic cancer cell line Hs766T cells caused by related compounds, it was found that only a small amount of cells died when 1.5μMPF-02341066 or lower concentration and 1.0μMARRY-142886 or lower concentration were used alone; When the ratio of 1.5μM PF-02341066+1.0μMARRY-142886 is used together, there is an 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 mitogen extracellular kinase (MEK) inhibitor, and application of the pharmaceutical composition in the preparation of medicaments for treating liver cancer, lung cancer, stomach cancer, intestinal 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 drugs for treating cancer, in particular to a pharmaceutical composition containing hepatocyte growth factor receptor inhibitors and mitogen extracellular kinase inhibitors and its application in the preparation of drugs for treating liver cancer , lung cancer, gastric cancer, bowel 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, primary liver cancer is a cancer that occurs in liver cells and intrahepatic bile duct epithelial cells, and is one of the most common m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/4545A61P35/00A61K31/4164
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG