Pharmaceutical composition containing amlexanox and mTOR inhibitor and application of pharmaceutical composition

A technology of aminolenol and a composition, which is applied in the field of pharmaceutical compositions containing aminolenol and mTOR inhibitors, can solve the problems of increased incidence of thrombosis events in patients with AS, increased risk of thrombosis, etc., and achieves rapid endothelial growth. It has the effect of reducing the incidence of AS, and delaying cell senescence.

Active Publication Date: 2018-04-03
MICROPORT SINICA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented combination uses both an AMPLIX (amictive X-ray absorption) agent with specific properties like being able to reduce calcium levels or block certain enzymes involved in inflammation process while also reducing tumor growth by targeting key molecules associated with this pathway called MTPs (methylthiolarginine).

Problems solved by technology

This patented technical problem addressed in this patent relates to improving the performance and safety profile of certain compounds called triprolinide analogs due to their ability to suppress both nausea/cough responses during experimental treatments aimed at reducing symptoms like painfulness caused by chemotherapies and radiation therapy. These modifications include adding alkali metal salts into medications containing these molecules, modifying them themselves, introducing new ones, exploring novel ways to modify existing methods, developing effective agents based upon these mechanisms, finding out potential applications in medicine preparative processes including gene regulations, stem cell culture, angiogenesis, cardiac disease modelings, and brain function testing.

Method used

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  • Pharmaceutical composition containing amlexanox and mTOR inhibitor and application of pharmaceutical composition
  • Pharmaceutical composition containing amlexanox and mTOR inhibitor and application of pharmaceutical composition
  • Pharmaceutical composition containing amlexanox and mTOR inhibitor and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1 Growth inhibitory effect on non-small cell lung cancer (NSCLC) cell line A549

[0083] 1) A549 cells were treated with a certain concentration of rapamycin for 72 hours, and the growth inhibitory effect of rapamycin alone on the non-small cell lung cancer (NSCLC) cell line A549 was investigated. The results are shown in Table 1.

[0084] Table 1

[0085] Rapamycin Concentration

growth inhibition ratefa

1nM

2.7％

5nM

12.5％

10nM

34.6％

20nM

43.7％

[0086] 2) A549 cells were treated with a certain concentration of amlexanox for 72 hours, and the growth inhibitory effect of amlexanox alone on the non-small cell lung cancer (NSCLC) cell line A549 was investigated. The results are shown in Table 2.

[0087] Table 2

[0088] Amlexanox Concentration

growth inhibition ratefa

0.1μM

0.9％

0.5μM

1.3％

1μM

5.5％

2μM

19.3％

[0089] 3) A549 cells were treat...

Embodiment 2

[0092] Example 2 Growth inhibitory effect on non-small cell lung cancer (NSCLC) cell line H460

[0093] 1) Treat H460 cells with a certain concentration of rapamycin for 72 hours, and investigate the growth inhibitory effect of rapamycin alone on the non-small cell lung cancer (NSCLC) cell line H460. The results are shown in Table 4.

[0094] Table 4

[0095] Rapamycin Concentration

growth inhibition ratefa

1nM

5.2％

5nM

9.8％

10nM

44.4％

20nM

51.3％

[0096] 2) The H460 cells were treated with a certain concentration of amlexanox for 72 hours, and the growth inhibitory effect of amlexanox alone on the non-small cell lung cancer (NSCLC) cell line H460 was investigated. The results are shown in Table 5.

[0097] table 5

[0098] Amlexanox Concentration

growth inhibition ratefa

0.1μM

1.5％

0.5μM

1.7％

1μM

4.6％

2μM

11.0％

[0099] 3) Treat H460 cells with a certai...

Embodiment 3

[0103] Example 3 Growth inhibitory effect on human gastric cancer cell line MGC-803

[0104] 1) MGC-803 cells were treated with a certain concentration of everolimus for 72 hours, and the inhibitory effect of everolimus alone on the growth of human gastric cancer cell line MGC-803 was investigated. The results are shown in Table 7.

[0105] Table 7

[0106] Everolimus concentration

growth inhibition ratefa

1nM

2.7％

5nM

3.5％

10nM

9.6％

20nM

15.1％

[0107] 2) MGC-803 cells were treated with a certain concentration of amlexanox for 72 hours, and the inhibitory effect of amlexanox alone on the growth of human gastric cancer cell line MGC-803 was investigated. The results are shown in Table 8.

[0108] Table 8

[0109] Amlexanox Concentration

growth inhibition ratefa

0.1μM

2.2％

0.5μM

3.4％

1μM

7.1％

2μM

7.8％

[0110] 3) MGC-803 cells were treated with a certain ...

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PUM

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Abstract

The invention particularly relates to a pharmaceutical composition containing amlexanox and an mTOR inhibitor and an application of the pharmaceutical composition. A surprising activity is displayed through the combined use of the amlexanox and the mTOR inhibitor; therefore, the invention provides the pharmaceutical composition, an interventional medical instrument applied to percutaneous coronaryintervention as well as applications in preparing medicines for preventing and treating angiostegnosis, vasculopathy and main coronary artery disease in patients with ischemic heart disease, acute occlusion or near occlusion in a PTCA operation, pathological change of PTCA significant residual stenosis or postoperative coronary restenosis disease and for preventing and treating benign or malignant tumors, epidermal hyperplasia, psoriasis or prostatic hyperplasia. The amlexanox and the mTOR inhibitor can take a synergistic activity in cell inhibition and cancer treatment; meanwhile, cell agingcan be delayed, and the AS occurrence rate and the thrombus occurrence rate, in comparison with that of independent use of the mTOR inhibitor, can be reduced; and rapid endothelialization of blood vessels can be promoted.

Description

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Claims

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Application Information

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Owner MICROPORT SINICA CO LTD
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