Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Novel pharmaceutical application of apatinib or pharmaceutically acceptable salt thereof

A technology of apatinib and medicinal salt, applied in the field of drug application, can solve the problem that there is no research report on apatinib MPM, and achieve the effects of clear drug action mechanism, good safety and outstanding curative effect

Inactive Publication Date: 2020-10-16
BEIJING SHIJITAN HOSPITAL CAPITAL MEDICAL UNIVERSTY
View PDF9 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] There is no research report on the treatment of MPM with apatinib and its pharmaceutically acceptable salts

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Novel pharmaceutical application of apatinib or pharmaceutically acceptable salt thereof
  • Novel pharmaceutical application of apatinib or pharmaceutically acceptable salt thereof
  • Novel pharmaceutical application of apatinib or pharmaceutically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: Apatinib mesylate inhibits viability and proliferation of malignant peritoneal mesothelioma cells

[0037] Experimental method: The effect of apatinib mesylate on the viability and proliferation of MPM cells was verified by the CCK8 assay; MPM cells in the logarithmic growth phase were taken, and the cell concentration was adjusted to 1×10 5 / mL, add 50 μL of cell suspension or medium to the 96-well plate, and after the cells adhere to the wall, set up the blank control group and the apatinib mesylate group with different concentrations (0, 12.5, 25, 50, 100 μM respectively) ), incubate for 24, 48, and 72 hours, and use the CCK8 kit to detect the proliferation of MPM cells in each group (the specific steps are operated according to the instructions of the kit).

[0038] The result is as figure 2 Shown: (A) Different concentrations of apatinib mesylate can inhibit the proliferation of MPM cells; (B) apatinib mesylate can inhibit the viability of MPM cells; (...

Embodiment 2

[0041] Example 2: Apatinib mesylate affects MPM cell cycle progression

[0042] Experimental method: The effect of apatinib mesylate on the cell cycle of MPM was analyzed by flow cytometry; the cell concentration was adjusted to 3×10 6 / mL, inoculated in a 6-well plate with 1 mL, set up blank control group and apatinib mesylate group (concentration: 50 μM), cultured for 24 and 48 hours respectively, and used PI kit to detect apatinib mesylate according to the instructions. Effects of tinib on the cell cycle of MPM.

[0043] The result is as image 3 Shown: (A) MPM cells cultured for 24 hours, the percentage of cells in each phase of the cycle; (B) 50 μM apatinib mesylate acted on MPM cells for 24 hours, the percentage of cells in each phase of the cycle; compared with the control group , cells in G1 phase increased, cells in G2 phase decreased; (C) MPM cells were cultured for 48 hours, the percentage of cells in each phase of the cycle; (D) 50 μM apatinib mesylate was applie...

Embodiment 3

[0044] Example 3: Scratch test to verify the effect of apatinib mesylate on the movement and migration of MPM cells

[0045] Experimental method: adjust the cell concentration to 1×10 6 / mL, add 80 μL to the 6-well plate, after the cells adhere to the wall, scratch the cell surface with the tip of the 200 μL sampler perpendicular to the cell surface, after light washing with PBS, replace the serum-free DMEM medium, set blank control, solvent control and methanesulfonate After culturing for 24 hours in the apatinib group (concentrations of 25 and 50 μM, respectively), the cell migration rate of each group was calculated.

[0046] The result is as Figure 4 Shown: (A1) and (A2) are the migration status of MPM cells in the blank control group at 0h and 24h respectively; (B1) and (B2) are the migration status of 25μM apatinib mesylate at 0h and 24h respectively; (C1) , (C2) 50μM apatinib mesylate 0h and 24h cell migration respectively; (D) cell migration rate of four groups. De...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a novel pharmaceutical application of apatinib or a pharmaceutically acceptable salt thereof, in particular to an application of apatinib or a pharmaceutically acceptable saltthereof in preparation of a medicine for treating malignant mesothelioma. The in-vitro test result shows that apatinib mesylate inhibits MPM cell proliferation and activity, affects the G2 / M phase ofthe MPM cell cycle process and remarkably inhibits MPM cell movement and migration; an in-vivo test result shows that the apatinib mesylate obviously reduces the ePCI score and has no influence on the body weight of nude mice. The apatinib has no histological toxicity to lung, spleen, kidney and gastrointestinal tract, only has focal lymphocyte infiltration in liver and myocardial tissues, and has an obvious effect of down-regulating NPM2 gene expression. The new application of apatinib or the pharmaceutically acceptable salt thereof provided by the invention provides an important theoreticalbasis for application of apatinib or the pharmaceutically acceptable salt thereof in treatment of malignant mesothelioma, widens the treatment range of the drug, and provides a new drug solution fortreatment of malignant mesothelioma.

Description

technical field [0001] The invention belongs to the technical field of medicine application, and in particular relates to a new medicine application of apatinib or a pharmaceutically acceptable salt thereof. Background technique [0002] The mesothelium is a thin film of epithelial cells that covers the surfaces of all body organs and cavities, such as the chest and abdomen. Mesothelioma is an aggressive tumor that invades the mesothelium and comes in four distinct types: pleural mesothelioma in 75% of cases, peritoneal mesothelioma in 10% to 20% of cases, and cardiac mesothelioma in 1% of cases. Mesothelioma, less than 1% of cases are testicular mesothelioma. Between 2,400 and 2,800 people are diagnosed with mesothelioma each year, according to a 2017 report from the U.S. Centers for Disease Control. People who have been in contact with or have been exposed to asbestos are at the highest risk of developing mesothelioma. Mesothelioma is extremely insidious and has usually...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/444A61P35/00
CPCA61K31/444A61P35/00
Inventor 李雁杨智冉陈谦杜雪梅
Owner BEIJING SHIJITAN HOSPITAL CAPITAL MEDICAL UNIVERSTY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com