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Application of pimavanserin tartrate in preparation of drug for treating glioma

A technology of pimavanserin and tartrate is applied in the application field of preparing drugs for treating glioma, can solve the problems of reduced curative effect and drug resistance of recurrent tumors, and achieves inhibition of proliferation and migration and strong anti-GBM activity. Effect

Active Publication Date: 2021-03-16
SHANDONG NORMAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, temozolomide is a commonly used first-line drug in chemotherapy, but long-term use is prone to drug resistance, especially for recurrent tumors with reduced curative effect

Method used

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  • Application of pimavanserin tartrate in preparation of drug for treating glioma
  • Application of pimavanserin tartrate in preparation of drug for treating glioma
  • Application of pimavanserin tartrate in preparation of drug for treating glioma

Examples

Experimental program
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Embodiment

[0048] Found that pimavanserin tartrate is a highly active NFAT signaling pathway inhibitor

[0049] In this example, 93 drug molecules covering different research fields were selected from the marketed drug compound library TargetMol-Approved Drug Screening Library as the compound library for screening, and were screened for NFAT signaling pathway inhibitory activity. The specific operation is as follows: HeLa cells stably transfected with NFAT1-GFP were inoculated into glass-bottom dishes and cultured overnight. Add 93 drug molecules to the cells at a final concentration of 100 μM and incubate for 30 min. Add 1 μM TG and 1 mM Ca to each dish 2+ , and incubate for 20 minutes. Subsequently, gently wash twice with PBS, and fix the cells with 4% paraformaldehyde (PFA) (1000 μL per dish) for 15 minutes at room temperature, then gently wash twice with PBS, and add 1000 μL of PBS. Imaging was performed using a Lecia SP8 laser scanning confocal microscope system. In this experim...

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Abstract

The invention relates to the technical field of medicines, in particular to application of pimavanserin tartrate in preparation of a drug for treating glioma, the glioma is polymorphic glioblastoma, and the application for treating glioma at least has any one or more of the following uses: (a) inhibiting the proliferation of glioma cells; (b) inhibiting the migration of glioma cells; (c) arrestingthe tumor cell cycle at G1 / S phase; and (d) inhibiting the growth of intracranial tumor cells in situ. The pimavanserin tartrate is found to be an effective NFAT signal pathway inhibitor, can inhibitE2F and MYC signal pathways and ATR and AuroraA / B signal pathways in tumor cells at the same time, has high anti-GBM activity in vivo, can effectively penetrate through a blood brain barrier (BBB) toenter the brain, can effectively inhibit growth of intracranial tumors in situ through oral administration, and is convenient to use. The invention provides a novel therapeutic drug for treating GBMtumors, which has important clinical significance.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of pimavanserin tartrate in the preparation of drugs for treating glioma. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Glioma is the most common primary intracranial tumor originating from the neuroepithelium, accounting for about 40%-50% of brain tumors. Glioblastoma multiforme (GBM) belongs to grade IV gliomas, accounting for about 50% of gliomas. Even with timely surgical resection, radiotherapy and chemotherapy treatment after diagnosis, the average survival period of patients is only 15-17 months. GBM can occur at any age, and has become the second m...

Claims

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Application Information

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IPC IPC(8): A61K31/4468A61P35/00
CPCA61K31/4468A61P35/00
Inventor 唐波刘真真刘晓宁李平李红丽
Owner SHANDONG NORMAL UNIV
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