Suppr超能文献

双重药物再利用:以萨拉替尼为例。

Dual Drug Repurposing: The Example of Saracatinib.

作者信息

Ramos Raquel, Vale Nuno

机构信息

PerMed Research Group, Center for Health Technology and Services Research (CINTESIS), Rua Doutor Plácido da Costa, 4200-450 Porto, Portugal.

CINTESIS@RISE, Faculty of Medicine, University of Porto, Alameda Professor Hernâni Monteiro, 4200-319 Porto, Portugal.

出版信息

Int J Mol Sci. 2024 Apr 22;25(8):4565. doi: 10.3390/ijms25084565.

Abstract

Saracatinib (AZD0530) is a dual Src/Abl inhibitor initially developed by AstraZeneca for cancer treatment; however, data from 2006 to 2024 reveal that this drug has been tested not only for cancer treatment, but also for the treatment of other diseases. Despite the promising pre-clinical results and the tolerability shown in phase I trials, where a maximum tolerated dose of 175 mg was defined, phase II clinical data demonstrated a low therapeutic action against several cancers and an elevated rate of adverse effects. Recently, pre-clinical research aimed at reducing the toxic effects and enhancing the therapeutic performance of saracatinib using nanoparticles and different pharmacological combinations has shown promising results. Concomitantly, saracatinib was repurposed to treat Alzheimer's disease, targeting Fyn. It showed great clinical results and required a lower daily dose than that defined for cancer treatment, 125 mg and 175 mg, respectively. In addition to Alzheimer's disease, this Src inhibitor has also been studied in relation to other health conditions such as pulmonary and liver fibrosis and even for analgesic and anti-allergic functions. Although saracatinib is still not approved by the Food and Drug Administration (FDA), the large number of alternative uses for saracatinib and the elevated number of pre-clinical and clinical trials performed suggest the huge potential of this drug for the treatment of different kinds of diseases.

摘要

萨拉卡替尼(AZD0530)是一种双重Src/Abl抑制剂,最初由阿斯利康公司开发用于癌症治疗;然而,2006年至2024年的数据显示,这种药物不仅已被测试用于癌症治疗,还用于治疗其他疾病。尽管临床前结果很有前景,且在I期试验中显示出耐受性(其中定义了最大耐受剂量为175毫克),但II期临床数据表明,该药物对几种癌症的治疗作用较低,且不良反应发生率较高。最近,旨在使用纳米颗粒和不同药物组合降低萨拉卡替尼的毒性作用并提高其治疗性能的临床前研究已显示出有前景的结果。与此同时,萨拉卡替尼被重新用于治疗阿尔茨海默病,靶向Fyn。它显示出了出色的临床效果,且所需的每日剂量低于为癌症治疗定义的剂量,分别为125毫克和175毫克。除了阿尔茨海默病外,这种Src抑制剂还针对其他健康状况进行了研究,如肺纤维化和肝纤维化,甚至还研究了其镇痛和抗过敏功能。尽管萨拉卡替尼仍未获得美国食品药品监督管理局(FDA)的批准,但萨拉卡替尼的大量替代用途以及所进行的大量临床前和临床试验表明,这种药物在治疗各种疾病方面具有巨大潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1172/11050334/b10c9751ad24/ijms-25-04565-g001.jpg

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验