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.
目前研究已经发现神经肽（SP）/神经激肽1受体（NK-1R）拮抗剂系统参与了包括2019冠状病毒病（COVID-19）症状在内的多种人体生理疾病。肿瘤学领域的最新研究表明：NK-1R的上调和SP/NK-1R系统的激活与多种癌症类型的进展和不良临床预后之间存在复杂的相关性，使用NK-1R拮抗剂来调节SP/NK-1R系统可成为一种潜在的广谱抗肿瘤策略。本文综述了NK-1R拮抗剂在人体生理疾病和癌症治疗中的最新应用和潜力以及相关机制，总结了改善NK-1R拮抗剂生物利用度和药效的策略（如固体分散系统、纳米化、纳米封装等），同时探讨了在放射药物治疗中，阿瑞匹坦作为放射配体受体以靶向过表达NK-1R的肿瘤疗法。此外，本文还总结了NK-1R拮抗剂与其他药物的协同效应，为NK-1R拮抗剂的创新应用提供了参考。.
目前研究已经发现神经肽（SP）/神经激肽1受体（NK-1R）拮抗剂系统参与了包括2019冠状病毒病（COVID-19）症状在内的多种人体生理疾病。肿瘤学领域的最新研究表明：NK-1R的上调和SP/NK-1R系统的激活与多种癌症类型的进展和不良临床预后之间存在复杂的相关性，使用NK-1R拮抗剂来调节SP/NK-1R系统可成为一种潜在的广谱抗肿瘤策略。本文综述了NK-1R拮抗剂在人体生理疾病和癌症治疗中的最新应用和潜力以及相关机制，总结了改善NK-1R拮抗剂生物利用度和药效的策略（如固体分散系统、纳米化、纳米封装等），同时探讨了在放射药物治疗中，阿瑞匹坦作为放射配体受体以靶向过表达NK-1R的肿瘤疗法。此外，本文还总结了NK-1R拮抗剂与其他药物的协同效应，为NK-1R拮抗剂的创新应用提供了参考。
Keywords: Bioavailability; Nanoencapsulation; Neurokinin-1 receptor (NK-1R) antagonist; Pathophysiological disorder; Synergistic therapy; Tumor target.