曲曲维林和达那韦在转化医学中的应用综述

Mariana Pereira, Nuno Vale
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摘要

这篇综合综述探讨了两种抗逆转录病毒药物,Etravirine (ETV)和Darunavir (DRV),一种非核苷逆转录酶抑制剂和蛋白酶抑制剂,通常用于人类免疫缺陷病毒(HIV)感染治疗,通常相互联合。介绍了这两种药物的药代动力学特性以及两种药物联合使用的临床试验。本文还探讨了这两种药物可能用于其他疾病的重新用途,药物重新用途是应对全球健康挑战的一个重要因素。DRV被广泛研究用于治疗COVID-19以及其他感染,如念珠菌病和隐球菌病,而ETV被证明可有效阻止寨卡病毒脑感染。研究还发现,ETV在体外对卵巢癌和肿瘤分子如前梯度蛋白2同源物(AGR2)和酪蛋白激酶1 (CK1ε)具有特殊的抑制作用,而DRV对人乳酸脱氢酶a (LDHA)具有硅酸抑制作用,诱导胃蛋白酶的体外和体内抑制,从而抑制咽喉癌和下咽癌的发生。在这项工作中强调了新药物开发方法的重要性,以及抗逆转录病毒药物ETV和DRV在病毒性和非病毒性疾病中的新治疗用途的巨大潜力。
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A Review Concerning the Use of Etravirine and Darunavir in Translational Medicine
This comprehensive review explores two antiretroviral drugs, Etravirine (ETV) and Darunavir (DRV), a non-nucleoside reverse transcriptase inhibitor and a protease inhibitor, that are commonly used in human immunodeficiency virus (HIV) infection treatment, often in combination with each other. The pharmacokinetic properties of these drugs are covered as well as the clinical trials of these two drugs combined. This paper also delves into the possible repurposing of these two drugs for other diseases, with drug repurposing being a significant factor in addressing global health challenges. DRV was extensively studied for treating COVID-19, as well as other infections, such as candidiasis and cryptococcosis, while ETV proved to be efficient in hampering Zika virus brain infection. The focus on cancer repurposing is also explored, with the results revealing that ETV has a particular inhibitory effect on ovarian cancer in vitro and on cancer molecules, such as anterior gradient protein 2 homolog (AGR2) and casein kinase 1 (CK1ε), and that DRV has an in silico inhibitory effect on human lactate dehydrogenase A (LDHA) and induces the in vitro and in vivo inhibition of pepsin, consequent laryngopharyngeal reflux, and possible laryngeal and hypopharyngeal carcinomas. The significance of fresh methods of drug development is emphasized in this work, as is the enormous potential for new therapeutic uses of the antiretroviral drugs ETV and DRV in viral and non-viral disorders.
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来源期刊
Journal of International Translational Medicine
Journal of International Translational Medicine MEDICINE, RESEARCH & EXPERIMENTAL-
自引率
0.00%
发文量
317
审稿时长
8 weeks
期刊介绍: Journal of International Translational Medicine (JITM, ISSN 2227-6394), founded in 2012, is an English academic journal published by Journal of International Translational Medicine Co., Ltd and sponsored by International Fderation of Translational Medicine. JITM is an open access journal freely serving to submit, review, publish, read and download full text and quote. JITM is a quarterly publication with the first issue published in March, 2013, and all articles published in English are compiled and edited by professional graphic designers according to the international compiling and editing standard. All members of the JITM Editorial Board are the famous international specialists in the field of translational medicine who come from twenty different countries and areas such as USA, Britain, France, Germany and so on.
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