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

A hepatocyte growth factor and receptor inhibitor technology, which is applied in the field of pharmaceutical compositions containing hepatocyte growth factor receptor inhibitors and mitogen extracellular kinase inhibitors and their uses, can solve the problem of high toxicity and patient discomfort. Tolerance and other issues

Inactive Publication Date: 2010-02-24
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,

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 used together at a lower concentration (1.0μM PF-02341066+0.25μM ARRY-142886), there is an obvious synergistic effect, resulting in About 60% of cancer cells died; when the two were combined at the ratio of 2.0μM PF-02341066+0.5μM ARRY-142886, a more obvious synergistic effect was produced, resulting in about 100% of cancer cell death.

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 investigating the death of pancreatic cancer cell line AsPC-1 cells caused by related compounds, it was found that only a small amount of cells died when 1.5 μM PF-02341066 or lower concentration and 0.5 μM ARRY-142886 or lower concentration were used alone; Even if the concentration of single drug is increased to 2.0μM PF-02341066 or 1.0μM ARRY-142886, only about 15-20% of the cells die; ) produced an obvious synergistic effect, resulting in the death of about 60% of cancer cells; when the two were used together at the ratio of 2.0μMPF-02341066+1.0μM ARRY-142886, a more obvious synergistic effect was produced, resulting in about 90% of cancer cells cell death.

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 investigating the death of pancreatic cancer cell line Hs766T cells caused by related compounds, it was found that when 1.5 μM PF-02341066 or lower concentration and 1.0 μM ARRY-142886 or lower concentration were used alone, only a small amount of cell death was found; When the two are combined at the ratio of 1.5μM PF-02341066+1.0μM ARRY-142886, 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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IPC IPC(8): A61K45/06A61K31/4545A61P35/00A61K31/4164
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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