Application of axitinib and PX-478 in treatment of nasopharyngeal carcinoma

A PX-478, 1. PX-478 technology, used in medical preparations containing active ingredients, pharmaceutical formulations, peptide/protein components, etc., can solve the problem of decreased white blood cell count, odorless or stale, increased, mucosal congestion, redness and swelling and other problems, to achieve good application prospects, significant curative effects, and significant therapeutic effects.

Active Publication Date: 2018-02-16
SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, radiation therapy may produce many complications: (1) Systemic reactions: including fatigue, dizziness, loss of appetite, nausea, vomiting, tasteless or bad taste in the mouth, insomnia or drowsiness, etc.
Individual patients may have blood changes, especially the decrease in white blood cell count; (2) Local reactions: including skin, mucous membrane, and salivary gland reactions; skin reactions manifest as dry dermatitis or even wet dermatitis, and mucosal reactions manifest as nasopharyngeal and oropharyngeal mucosal hyperemia , edema, exudation and accumulation of secretions, etc. In a small number of patients, parotid gland swelling can occur after 2Gy irradiation. When 40Gy is irradiated, the secretion of saliva is significantly reduced, and the secretion of oral mucosa is increased at the same time. Difficulty eating; ③Radiotherapy regression: mainly temporomandibular joint dysfunction, soft tissue atrophy and fibrosis, radiation caries, radiation-induced jaw osteomyelitis, and radiation-induced encephalomyelopathy, and there is no proper way to reverse it
[0004] Moreover, clinically, most of the patients are in the middle and late stage when they go to the doctor. For the cases of less differentiated cancer, late course of disease and recurrence after radiotherapy, recurrence often occurs even after regular treatment of nasopharyngeal carcinoma such as surgery, radiotherapy and chemotherapy. and transfer

Method used

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  • Application of axitinib and PX-478 in treatment of nasopharyngeal carcinoma
  • Application of axitinib and PX-478 in treatment of nasopharyngeal carcinoma
  • Application of axitinib and PX-478 in treatment of nasopharyngeal carcinoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Effect of axitinib on tube formation of vascular endothelial cells

[0031] 1. Experimental materials

[0032] (1) Drug: Axitinib, its chemical formula is: C22H18N4OS, and its CAS number is: 319460-85-0

[0033] (2) Vascular endothelial cells: human umbilical vein endothelial cells (HUVEC)

[0034] (3) Commercially available matrigel.

[0035] 2. Experimental grouping

[0036] (1) Control group: blank control, that is, HUVEC without any drug treatment.

[0037] (2) Experimental group: HUVEC were treated with axitinib.

[0038] 3. Angiogenesis assay to detect the effect of axitinib on HUVEC tube formation

[0039] (1) After thawing Matrigel at -20°C, spread 30 μL on a 96-well plate and place in a 37°C incubator for 30 minutes;

[0040] (2) Digest HUVEC cells in the logarithmic growth phase with trypsin and resuspend in the complete medium, take 200 μL (containing 5×10 4 Cells) were spread evenly on Matrigel matrigel in 96-well plate;

[0041] (3) Add ax...

Embodiment 2

[0045] Example 2 Effect of PX-478 on EBV-positive nasopharyngeal carcinoma cells VM

[0046] 1. Experimental materials

[0047] (1) Drug: PX-478, its chemical formula is: C13H20Cl4N2O3, and its CAS number is: 685898-44-6

[0048] (2) Cancer cells: EBV positive nasopharyngeal carcinoma cells (HNE1-EBV, CNE2-EBV and TWO3-EBV)

[0049] (3) Commercially available matrigel.

[0050] 2. Experimental grouping

[0051] (1) Control group: blank control, that is, the cancer cells were not treated with any drugs.

[0052] (2) Experimental group: Cancer cells were treated with PX-478.

[0053] 3. Angiogenesis assay to detect the effect of PX-478 on EBV-positive nasopharyngeal carcinoma cells VM

[0054] (1) After thawing Matrigel at -20°C, spread 30 μL on a 96-well plate and place in a 37°C incubator for 30 minutes;

[0055] (2) Digest the HNE1-EBV, CNE2-EBV and TWO3-EBV cells in the logarithmic growth phase with trypsin and resuspend in the complete medium, take 200 μL (containing ...

Embodiment 3

[0060] Example 3 Effect of axitinib combined with PX-478 on EBV-positive nasopharyngeal carcinoma cell xenografts

[0061] 1. Experimental materials

[0062](1) Drugs: Axitinib and PX-478

[0063] (2) Cancer cells: EBV-positive nasopharyngeal carcinoma cells (CNE2-EBV)

[0064] (3) Commercially purchased nude mice.

[0065] 2. Experimental grouping

[0066] (1) Control group: blank control, that is, the cancer cells were not treated with any drugs.

[0067] (2) Axitinib group: Axitinib was used to treat EBV-positive nasopharyngeal carcinoma cells.

[0068] (3) PX-478 group: EBV-positive nasopharyngeal carcinoma cells were treated with PX-478.

[0069] (4) Axitinib + PX-478 group: EBV-positive nasopharyngeal carcinoma cells were treated with axitinib and PX-478 at the same time.

[0070] 3. The effect of axitinib or / and PX-478 on EBV-positive nasopharyngeal carcinoma cell xenografts was detected by subcutaneous tumor formation experiment in nude mice

[0071] (1) with 5×...

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PUM

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Abstract

The invention discloses PX-478, and an application of combined use of axitinib and PX-478 in treatment of nasopharyngeal carcinoma. The PX-478 is discovered to significantly inhibit formation of VM ofnasopharyngeal carcinoma cells, inhibit the growth of transplantation tumor and have a significant curative effect on nasopharyngeal carcinoma for a first time. At the same time, a research discoversthat the axitinib and PX-478 combined medication achieves synergistic effect and has a more significant curative effect on nasopharyngeal carcinoma. The invention not only provides the new application of axitinib and PX-478, but also provides a new treatment medication regimen for treatment of nasopharyngeal carcinoma, and has a good application prospect in prevention and treatment of nasopharyngeal carcinoma.

Description

technical field [0001] The invention belongs to the technical field of medicine. More specifically, it relates to the application of Axitinib and PX-478 in the treatment of nasopharyngeal carcinoma. Background technique [0002] Nasopharyngeal carcinoma is one of the malignant tumors in my country, and its incidence rate is the first among malignant tumors of the ear, nose and throat. Most nasopharyngeal carcinomas are moderately sensitive to radiotherapy, and radiotherapy is the first choice for the treatment of nasopharyngeal carcinoma. [0003] However, radiation therapy may produce many complications: (1) Systemic reactions: including fatigue, dizziness, loss of appetite, nausea, vomiting, tasteless or bad taste in the mouth, insomnia or drowsiness, etc. Individual patients may have blood changes, especially the decrease in white blood cell count; (2) Local reactions: including skin, mucous membrane, and salivary gland reactions; skin reactions manifest as dry dermatit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K31/195A61P35/00
CPCA61K31/195A61K31/4439A61K2300/00
Inventor 向橦曾益新冯琳马文龙冯启胜何贵平
Owner SUN YAT SEN UNIV
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