Advances in the research and application of neurokinin-1 receptor antagonists  

作　　者：Xiangyu HONG Junjie MA Shanshan ZHENG Guangyu ZHAO Caiyun FU 

机构地区：[1]College of Life Sciences and Medicine,Zhejiang Sci-Tech University,Hangzhou,310018,China

出　　处：《Journal of Zhejiang University-Science B(Biomedicine & Biotechnology)》2024年第2期91-105,共15页浙江大学学报（英文版）B辑（生物医学与生物技术）

基　　金：This work was supported by the Zhejiang Provincial Natural Science Foundation of China(No.LD22H310004);the“Pioneer”and“Leading Goose”R&D Program of Zhejiang(No.2022C03005),China.

摘　　要：Recently,the substance P(SP)/neurokinin-1 receptor(NK-1R)system has been found to be involved in various human pathophysiological disorders including the symptoms of coronavirus disease 2019(COVID-19).Besides,studies in the oncological field have demonstrated an intricate correlation between the upregulation of NK-1R and the activation of SP/NK-1R system with the progression of multiple carcinoma types and poor clinical prognosis.These findings indicate that the modulation of SP/NK-1R system with NK-1R antagonists can be a potential broad-spectrum antitumor strategy.This review updates the latest potential and applications of NK-1R antagonists in the treatment of human diseases and cancers,as well as the underlying mechanisms.Furthermore,the strategies to improve the bioavailability and efficacy of NK-1R antagonist drugs are summarized,such as solid dispersion systems,nanonization,and nanoencapsulation.As a radiopharmaceutical therapeutic,the NK-1R antagonist aprepitant was originally developed as radioligand receptor to target NK-1R-overexpressing tumors.However,combining NK-1R antagonists with other drugs can produce a synergistic effect,thereby enhancing the therapeutic effect,alleviating the symptoms,and improving patients’quality of life in several diseases and cancers.

关 键 词：Neurokinin-1 receptor(NK-1R)antagonist Pathophysiological disorder Tumor target BIOAVAILABILITY NANOENCAPSULATION Synergistic therapy 

分 类 号：R318[医药卫生—生物医学工程]