Pharmaceutical composition containing amlexanox and mTOR inhibitor and application thereof

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

Active Publication Date: 2021-04-02
MICROPORT SINICA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The present invention provides a pharmaceutical composition containing amlexanox and mTOR inhibitors, which is used to solve the problem that the clinical application of mTOR inhibitors increases the incidence of AS and the risk of thrombotic events in patients

Method used

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  • Pharmaceutical composition containing amlexanox and mTOR inhibitor and application thereof
  • Pharmaceutical composition containing amlexanox and mTOR inhibitor and application thereof
  • Pharmaceutical composition containing amlexanox and mTOR inhibitor and application thereof

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 treated with a certain concentration of amlexano...

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 certain concentration of amlexanol combined with ...

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 concentration of amlexanox combined with a...

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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

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a pharmaceutical composition containing amlexanox and an mTOR inhibitor and application thereof. Background technique [0002] Amlexanox, common name: 2-Amino-7-isopropyl-5-oxo-5H[1]phenylpyranyl-[2,3,-b]-pyridine-3-carboxylbenzoic acid , also known as CHX3673. English chemical name: 2-amimo-7-isopropyl-5-oxo-5H-[1]benzopyrano-[2,3,-b]pyridine-3-carboxylic acid. [0003] In the prior art, amlexonol is an allergic reaction mediator blocker, which stabilizes the cell membrane of mast cells and inhibits their degranulation, thereby preventing the release of allergic reaction mediators and having an anti-allergic effect. Amlexanol was synthesized for the first time in 1987 for the treatment of allergic bronchial asthma and later for allergic rhinitis. In 1996, Amlycanox was approved by the FDA for the treatment of oral ulcers. Its main pharmacological effect is to accelerate th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K31/436A61L31/16A61P35/00
CPCA61K31/436A61K45/06A61L31/16A61L2300/204A61L2300/416A61L2300/42A61L2300/606A61K2300/00
Inventor 陈陆李俊菲胡燕
Owner MICROPORT SINICA CO LTD
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