Advances in the research and application of neurokinin-1 receptor antagonists
- Author:
HONG XIANGYU
1
;
MA JUNJIE
;
ZHENG SHANSHAN
;
ZHAO GUANGYU
;
FU CAIYUN
Author Information
- Keywords: Neurokinin-1 receptor(NK-1R)antagonist; Pathophysiological disorder; Tumor target; Bioavailability; Nanoencapsulation; Synergistic therapy
- From: Journal of Zhejiang University. Science. B 2024;25(2):91-105
- CountryChina
- Language:Chinese
- Abstract: 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.
