VEGFR inhibitor and blood pressure reducing medicine composition and application thereof

A technology of a composition and antihypertensive drug, applied in the field of medicine, can solve the problems that the combination use has not received extensive attention, and the side effects of targeted drugs are less concerned, and achieve significant curative effect, broad research prospects, and the effect of reducing blood pressure elevation.

Inactive Publication Date: 2020-02-07
TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In recent years, a large number of studies have focused on the combination of targeted anticancer drugs, but the combination...

Method used

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  • VEGFR inhibitor and blood pressure reducing medicine composition and application thereof
  • VEGFR inhibitor and blood pressure reducing medicine composition and application thereof
  • VEGFR inhibitor and blood pressure reducing medicine composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Inhibitory effects of axitinib and losartan monomers and combined drugs on the growth of kidney cancer in the subcutaneous xenograft tumor model of Balb / c nude mice. The compounds in each group were administrated with 0.5% sodium carboxymethylcellulose suspension Administration for 15 days. Axitinib has two drug concentrations of low dose 30mg / kg and high dose 60mg / kg, and losartan is administered at 10mg / kg. The experimental results are shown in Table 1.

[0027] Table 1 Inhibitory effects of axitinib and losartan monomers and combined drugs on the growth of renal cell carcinoma

[0028]

[0029] It can be seen from the above results that axitinib has a significant inhibitory effect on the growth of renal cancer in a dose-dependent manner, and the combination of losartan will not significantly reduce its anti-tumor effect. Kidney cancer also has an inhibitory effect.

Embodiment 2

[0031] Effects of axitinib and losartan alone and in combination on skin vascular permeability (Miles test)

[0032] Axitinib (10mg / kg), losartan (10mg / kg) and its combination axitinib (10mg / kg) + losartan (10mg / kg) were administered to C57BL / 6N small Rats were injected with Evans blue dye through the tail vein. After anesthesia, both sides of the abdomen were shaved. PBS and 1% VEGFA were injected into the skin on both sides. After 4 hours, a vertical incision of about 3-4 cm was made from the lower abdomen to the chest with scissors. . Remove areas of dye accumulation. After the sample is dried, formamide is added to extract the Evans blue dye, and the absorbance value is detected.

[0033] The result is attached figure 1 As shown, it can be seen from the control group that VEGFA can significantly increase vascular permeability. This effect was blocked by the VCGFR inhibitor axitinib, which reduced VEGFA-induced hypervascular permeability, which is one of the mechanisms ...

Embodiment 3

[0035] Effects of axitinib and losartan alone and in combination on blood pressure in Wistar rats

[0036] Randomly select 8 7-week-old Wistar rats, 2 in each group, orally administer axitinib (25mg / kg), losartan (10mg / kg), axitinib (25mg / kg) + loxa Tan (10mg / kg) and control sodium carboxymethylcellulose, twice a day for 7 consecutive days. Changes in systolic blood pressure were monitored daily.

[0037] The results of the systolic blood pressure test on the 7th day are attached figure 2 As shown, compared with the control group, axitinib significantly increased the systolic blood pressure of rats by about 20%, and the combined administration of losartan significantly reduced the increase in blood pressure caused by axitinib.

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PUM

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Abstract

The invention relates to a VEGFR inhibitor and blood pressure reducing medicine composition. The composition is a composition of Axitinib and Losartan. The medicine composition lies in combined use ofAxitinib and Losartan, and in vivo experimentation on animals confirms that compared with single medicine of the Axitinib, the composition not only has notable treatment effects on carcinoma of kidney, but also notably reduces side effects of elevation of blood pressure, liver enzyme, elevation of serum creatinine caused by the Axitinib. The VEGFR inhibitor and blood pressure reducing medicine composition is controllable for side effects of antitumor drugs for targeting VEGFR, and a new research thought train is provided for clinical application of target medicines.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a composition of a VEGFR inhibitor and an antihypertensive drug and an application thereof. Background technique [0002] VEGFR (vascular endothelial growth factor receptor) plays an important role in the occurrence and development of blood vessels, especially in tumor blood vessels. VEGFR inhibitors have good effects and are widely used in anti-tumor therapy, especially in the treatment of renal cancer. At the same time, the application of VEGFR inhibitors is often accompanied by complications such as hypertension, bleeding, kidney injury, and elevated liver enzymes, which affect the prognosis and quality of life of cancer patients. [0003] Axitinib is an inhibitor targeting VEGFR1, 2, 3, which was approved by the US Food and Drug Administration (FDA) in 2012 compared with the second-line drug Sorafenib for kidney cancer, which significantly prolongs the progression-free surviv...

Claims

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Application Information

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IPC IPC(8): A61K31/4439A61K31/4178A61P35/00
CPCA61K31/4178A61K31/4439A61P35/00A61K2300/00
Inventor 滕玉鸥萨旭仁贵荣耀赵彩孔祥舜赵连波郝磊王栋郁彭
Owner TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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