CN107468691A - Application of the Axitinib in terms of nasopharyngeal carcinoma is treated - Google Patents
Application of the Axitinib in terms of nasopharyngeal carcinoma is treated Download PDFInfo
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- CN107468691A CN107468691A CN201710707337.XA CN201710707337A CN107468691A CN 107468691 A CN107468691 A CN 107468691A CN 201710707337 A CN201710707337 A CN 201710707337A CN 107468691 A CN107468691 A CN 107468691A
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- Prior art keywords
- axitinib
- nasopharyngeal carcinoma
- nasopharyngeal
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- medicine
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- 208000002454 Nasopharyngeal Carcinoma Diseases 0.000 title claims abstract description 46
- 206010061306 Nasopharyngeal cancer Diseases 0.000 title claims abstract description 41
- 201000011216 nasopharynx carcinoma Diseases 0.000 title claims abstract description 41
- RITAVMQDGBJQJZ-FMIVXFBMSA-N axitinib Chemical compound CNC(=O)C1=CC=CC=C1SC1=CC=C(C(\C=C\C=2N=CC=CC=2)=NN2)C2=C1 RITAVMQDGBJQJZ-FMIVXFBMSA-N 0.000 title claims abstract description 38
- 229960003005 axitinib Drugs 0.000 title claims abstract description 34
- 239000003814 drug Substances 0.000 claims abstract description 21
- 230000012010 growth Effects 0.000 claims abstract description 9
- 229940079593 drug Drugs 0.000 claims description 5
- 239000000463 material Substances 0.000 claims description 5
- 230000010261 cell growth Effects 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 3
- 239000007787 solid Substances 0.000 abstract description 2
- 210000004027 cell Anatomy 0.000 description 14
- 238000002474 experimental method Methods 0.000 description 8
- 201000011510 cancer Diseases 0.000 description 5
- 238000001959 radiotherapy Methods 0.000 description 5
- 238000002054 transplantation Methods 0.000 description 5
- 238000001514 detection method Methods 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 210000003556 vascular endothelial cell Anatomy 0.000 description 4
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 108010082117 matrigel Proteins 0.000 description 3
- 230000028327 secretion Effects 0.000 description 3
- 201000004624 Dermatitis Diseases 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
- 241000699666 Mus <mouse, genus> Species 0.000 description 2
- 241000699660 Mus musculus Species 0.000 description 2
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 description 2
- 102100024616 Platelet endothelial cell adhesion molecule Human genes 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 210000002889 endothelial cell Anatomy 0.000 description 2
- 210000004400 mucous membrane Anatomy 0.000 description 2
- 210000001989 nasopharynx Anatomy 0.000 description 2
- 238000011580 nude mouse model Methods 0.000 description 2
- 210000003681 parotid gland Anatomy 0.000 description 2
- 230000000149 penetrating effect Effects 0.000 description 2
- 230000005855 radiation Effects 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 210000001519 tissue Anatomy 0.000 description 2
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010013786 Dry skin Diseases 0.000 description 1
- 206010020565 Hyperaemia Diseases 0.000 description 1
- 206010024769 Local reaction Diseases 0.000 description 1
- 206010061307 Neck deformity Diseases 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 206010031252 Osteomyelitis Diseases 0.000 description 1
- 108010019160 Pancreatin Proteins 0.000 description 1
- 206010037764 Radiation myelopathy Diseases 0.000 description 1
- 238000011579 SCID mouse model Methods 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 230000037336 dry skin Effects 0.000 description 1
- 238000004043 dyeing Methods 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000003760 hair shine Effects 0.000 description 1
- 230000002055 immunohistochemical effect Effects 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 230000001678 irradiating effect Effects 0.000 description 1
- 208000025848 malignant tumor of nasopharynx Diseases 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 229940055695 pancreatin Drugs 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 238000002271 resection Methods 0.000 description 1
- 210000003079 salivary gland Anatomy 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 210000001738 temporomandibular joint Anatomy 0.000 description 1
- 238000010257 thawing Methods 0.000 description 1
- 210000003606 umbilical vein Anatomy 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of the Axitinib in terms of nasopharyngeal carcinoma is treated.Present invention firstly discovers that Axitinib can significantly inhibit the growth of nasopharyngeal carcinoma transplantable tumor, there is the effect of notable to nasopharyngeal carcinoma.The invention provides a kind of new application of Axitinib, also provides a kind of new medicine for the treatment of nasopharyngeal carcinoma, has good application prospect in terms of the preventing and treating of nasopharyngeal carcinoma.Moreover, Axitinib has been a kind of clinical application at present, there is solid clinical practice basis.
Description
Technical field
The invention belongs to pharmaceutical technology field.More particularly, to Axitinib（Axitinib）In treatment prescription for nasopharyngeal cancer
The application in face.
Background technology
Nasopharyngeal carcinoma is one of China's malignant tumour, and the incidence of disease is first of ear,nose ＆ throat malignant tumour.Nasopharyngeal carcinoma is multipair greatly to put
Penetrating treatment has Medium sensitivity, and radiotherapy is the preferred treatment method of nasopharyngeal carcinoma.
But radiotherapy may produce many complication：（1）General reaction：Including weak, dizzy, stomach receive decline,
Nausea and vomiting, flat feeling in the mouth or spoiled, insomnia or drowsiness etc..Blood change, especially leucocyte meter can occur for few patients
Number is reduced；（2）Local reaction：Reaction including skin, mucous membrane, salivary gland；Even it is moist that dermoreaction shows as dry skin dermatitis
Dermatitis, mucosa reaction shows as nasopharynx and oropharyngeal mucosae hyperemia, oedema, ooze out and secretion accumulates etc., the small number of patients parotid gland shines
Swelling of parotid gland can occur after penetrating 2Gy, when irradiating 40Gy, salivary secretion significantly reduces, while mucous membrane of mouth secretion increase, sticks
Film is congested, red and swollen, patient's dry, enters xerophagia difficulty；3. radiotherapy retreats disease：Mainly there are Temporomandibular joint and soft tissue to wither
Shrinkage fibers, radioactivity carious tooth and radiation osteomyelitis of jaw and radiation myelopathy, the appropriate method of reverse is there is no at present.
Moreover, clinically patient assessment when belonged to middle and advanced stage mostly, for compared with poor differentiated carcinoma, the course of disease is later and radiotherapy after
The case of recurrence, though after the regular means treatment of the nasopharyngeal carcinoma such as underwent operative, radiation and chemotherapy, also can be it occur frequently that recurrence and transfer.
The content of the invention
The technical problem to be solved in the present invention is the defects of overcoming existing treatment of nasopharyngeal carcinoma technology and deficiency, there is provided Yi Zhongxin
Treatment of nasopharyngeal carcinoma medicine.Present invention firstly discovers that Axitinib can significantly inhibit the growth of nasopharyngeal carcinoma transplantable tumor, to nasopharynx
Cancer has the effect of notable, in terms of the preventing and treating that can be applied to nasopharyngeal carcinoma.
It is an object of the invention to provide application of the Axitinib in terms of nasopharyngeal carcinoma is treated.
Above-mentioned purpose of the present invention is achieved through the following technical solutions：
The invention provides application of the Axitinib in terms for the treatment of medicine for nasopharyngeal is prepared.
Particularly preferably, the treatment medicine for nasopharyngeal refers to the medicine for suppressing nasopharyngeal carcinoma growth.
More specifically, the growth for suppressing nasopharyngeal carcinoma growth and referring to suppress nasopharyngeal carcinoma cell.
Furthermore it is preferred that the nasopharyngeal carcinoma is EBV positive nasopharyngeal carcinomas.Because clinically more than 98% Nasopharyngeal Carcinoma Patients are equal
Positive for EBV, therefore, present invention experiment is carried out by taking EBV positive nasopharyngeal carcinomas as an example.
Present invention also offers a kind of medicine for treating nasopharyngeal carcinoma, the medicine contains Axitinib.
Preferably, the medicine refers to the medicine for treating EBV positive nasopharyngeal carcinomas.
In addition, the medicine can also include medically acceptable auxiliary material or carrier, different formulations is prepared into, or and its
He is compounded medicament selection.
The invention has the advantages that：
The invention provides a kind of new application of Axitinib, the i.e. application in terms of nasopharyngeal carcinoma is treated.The present invention studies first
It was found that Axitinib can significantly inhibit the growth of nasopharyngeal carcinoma cell transplantable tumor, there is the effect of notable to nasopharyngeal carcinoma, in nasopharynx
There is good application prospect in terms of the preventing and treating of cancer.
Moreover, Axitinib has been a kind of clinical application at present, there is solid clinical practice basis.
Brief description of the drawings
Fig. 1 is influence of the Axitinib to vascular endothelial cell into pipe.
Fig. 2 is influence of the Axitinib to EBV positive nasopharyngeal carcinoma's cell transplantation knurl sizes.
Fig. 3 is the ImmunohistochemistryResults Results that Axitinib influences on EBV positive nasopharyngeal carcinoma's cell transplantations knurl.
Embodiment
The present invention is further illustrated below in conjunction with Figure of description and specific embodiment, but embodiment is not to the present invention
Limit in any form.Unless stated otherwise, the reagent of the invention used, method and apparatus routinely try for the art
Agent, method and apparatus.
Unless stated otherwise, following examples agents useful for same and material are purchased in market.
Found by the practical work of inventor team for many years, clinically more than 98% Nasopharyngeal Carcinoma Patients are EBV sun
Property, therefore, following examples experiment is presented by taking EBV positive nasopharyngeal carcinomas as an example.
Influence of the Axitinib of embodiment 1 to vascular endothelial cell into pipe
1st, experiment material
（1）Medicine：Axitinib, its chemical formula are：C22H18N4OS, No. CAS is：319460-85-0
（2）Vascular endothelial cell：Human umbilical vein endothelial cells（HUVEC）
（3）Matrigel matrigels purchased in market.
2nd, experiment packet
（1）Control group：Blank control, i.e. HUVEC are without any drug-treated.
（2）Experimental group：HUVEC is handled using Axitinib.
3rd, influence of the vascularization experiment detection Axitinib to HUVEC into pipe
（1）After -20 DEG C of defrostings of Matrigel matrigels, take 30 μ L to be laid in 96 orifice plates, be put in 37 DEG C of incubator 30min；
（2）Complete medium is resuspended after the HUVEC cells of exponential phase are digested with pancreatin, takes 200 μ L（Containing 5 × 104Carefully
Born of the same parents）Uniformly it is taped against on the Matrigel matrigels in 96 orifice plates；
（3）The Axitinib of 1000nM concentration is added, 37 DEG C of incubators are incubated 12h.
（4）Inverted microscope situation cell is into pipe situation.
4th, experimental result
As a result as shown in figure 1, after display is handled with Axitinib in Fig. 1, HUVEC official jargon is obviously reduced, and shows Axitinib
Vascular endothelial cell can be resisted into pipe.
Influence of the Axitinib of embodiment 2 to EBV positive nasopharyngeal carcinoma's cell transplantation knurls
1st, experiment material
（1）Medicine：Axitinib
（2）Cancer cell：EBV positive nasopharyngeal carcinoma's cells（CNE2-EBV）
（3）Nude mice purchased in market.
2nd, experiment packet
（1）Control group：Blank control, i.e. cancer cell are without any drug-treated.
（2）Axitinib group：EBV positive nasopharyngeal carcinoma's cells are handled using Axitinib.
3rd, nude mice by subcutaneous tests influence of the detection Axitinib to EBV positive nasopharyngeal carcinoma's cell transplantation knurls into knurl
（1）Respectively with 5 × 106EBV positive nasopharyngeal carcinoma's cells of numerical value（CNE2-EBV）It is implanted into 40 3~4 week old NOD/SCID
Mouse armpit is subcutaneous.It is randomly divided into 2 groups：Blank control group, Axitinib group.
（2）When hypodermic tumour size reaches 100~200mm3When, every mouse of Axitinib group gives 30mg/kg daily
Axitinib 2 times.
（3）The tumor size of detection in every 2 days, tumour forms difference between comparing each group.
（4）After 2 weeks, short neck puts to death mouse, tumor resection tissue, and neutral formalin is fixed, specimens paraffin embedding slices, row HE
Dyeing carries out histology, immunohistochemical experiment detection mark CD31, PAS expression.
3rd, experimental result
As a result as shown in Fig. 2 Axitinib can significantly resist the growth of EBV positive nasopharyngeal carcinoma's cell transplantation knurls.As Fig. 3 is immunized
Groupization result shows that the CD31 positive endothelial cells that Axitinib is resisted in tumor tissues form blood vessel.
Claims (7)
1. application of the Axitinib in terms for the treatment of medicine for nasopharyngeal is prepared.
2. application according to claim 1, it is characterised in that the treatment medicine for nasopharyngeal refers to suppress nasopharyngeal carcinoma growth
Medicine.
3. application according to claim 2, it is characterised in that the suppression nasopharyngeal carcinoma growth refers to suppress nasopharyngeal carcinoma cell
Growth.
4. according to any described application of claims 1 to 3, it is characterised in that the nasopharyngeal carcinoma is EBV positive nasopharyngeal carcinomas.
5. a kind of medicine for treating nasopharyngeal carcinoma, it is characterised in that contain Axitinib.
6. medicine according to claim 5, it is characterised in that the nasopharyngeal carcinoma is EBV positive nasopharyngeal carcinomas.
7. medicine according to claim 5, it is characterised in that also including medically acceptable auxiliary material or carrier.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710707337.XA CN107468691A (en) | 2017-08-17 | 2017-08-17 | Application of the Axitinib in terms of nasopharyngeal carcinoma is treated |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710707337.XA CN107468691A (en) | 2017-08-17 | 2017-08-17 | Application of the Axitinib in terms of nasopharyngeal carcinoma is treated |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107468691A true CN107468691A (en) | 2017-12-15 |
Family
ID=60600836
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710707337.XA Pending CN107468691A (en) | 2017-08-17 | 2017-08-17 | Application of the Axitinib in terms of nasopharyngeal carcinoma is treated |
Country Status (1)
| Country | Link |
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| CN (1) | CN107468691A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110724127A (en) * | 2019-11-29 | 2020-01-24 | 天津科技大学 | Synthetic method and anti-tumor application of seleno-axitinib |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644562A (en) * | 2013-11-23 | 2015-05-27 | 天津市汉康医药生物技术有限公司 | Axitinib composition and preparation method thereof |
-
2017
- 2017-08-17 CN CN201710707337.XA patent/CN107468691A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104644562A (en) * | 2013-11-23 | 2015-05-27 | 天津市汉康医药生物技术有限公司 | Axitinib composition and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| HUI EP等: ""Preclinical activity of axitinib and its associated change of serum biomarkers in nasopharyngeal carcinoma"", 《CANCER RES》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110724127A (en) * | 2019-11-29 | 2020-01-24 | 天津科技大学 | Synthetic method and anti-tumor application of seleno-axitinib |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20171215 |