摘要
南美锥虫病、美洲锥虫病是一种被忽视的热带病由寄生虫克氏锥虫。虽然感染者的数量有所减少,全世界约6-7万人感染。目前使用的化疗药物是有限的苯并咪唑和硝呋莫司。他们针对急性期,先天性传播和儿童慢性感染有效。但是,最近的临床试验显示在成人慢性感染的局限性,在治疗过程中出现的缺点。因此,有一个新的有效的,安全的和负担得起的药物,以针对这种复杂的疾病的迫切需要。有很高的期望,他们的唑类衍生物的出现在过去的十年是南美锥虫病的治疗最有前途的药物;然而,令人失望的结果到目前为止,在临床试验中证明的临床前和临床发展之间缺乏相关性。因此,从这些研究中获得的反馈应确定为解决这种疾病的药物发现过程中的一个路线图的出发点。为了应对这一挑战,记住药物靶形十分重要,这已经由专家小组和协调工作,涉及多学科网络不仅注重发现新的药物也加速了南美锥虫病的药物发现过程。
关键词: 南美锥虫病、锥虫药物发现、筛选级联,临床试验,目标产物简介,被忽视的热带病。
Current Medicinal Chemistry
Title:Challenges in Chagas Disease Drug Discovery: A Review
Volume: 23 Issue: 28
Author(s): Rocio Paucar, Elsa Moreno-Viguri, Silvia Pérez-Silanes
Affiliation:
关键词: 南美锥虫病、锥虫药物发现、筛选级联,临床试验,目标产物简介,被忽视的热带病。
摘要: Chagas disease or American trypanosomiasis is a neglected tropical disease caused by the parasite Trypanosoma cruzi. Although the number of infected individuals has decreased, about 6-7 million people are infected worldwide. The chemotherapy drugs currently used are limited to benznidazole and nifurtimox. They are effective in acute phase, congenital transmission and children with chronic infection; however, recent clinical trials have shown limitations in adults with chronic infection, presenting drawbacks during the treatment. Thus, there is an urgent need for new effective, safe and affordable drugs to fight against this complex disease. There were high expectations for azole derivatives as they appeared to be the most promising drugs for the treatment of Chagas disease during the last decade; however, the disappointing results obtained so far in clinical trials evidenced the lack of correlation between preclinical and clinical development. Therefore, the feedback obtained from these studies should define the starting point for addressing a roadmap for the drug discovery process in the fight against this disease. To tackle this challenge, it is important to keep in mind the drug target profile, already defined by panels of experts, and the coordinated work involving multi-disciplinary networks focusing not only on the discovery of new drugs but also on the standardization of the protocols that would allow acceleration in the Chagas disease drug discovery process.
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Cite this article as:
Rocio Paucar, Elsa Moreno-Viguri, Silvia Pérez-Silanes , Challenges in Chagas Disease Drug Discovery: A Review, Current Medicinal Chemistry 2016; 23 (28) . https://dx.doi.org/10.2174/0929867323999160625124424
DOI https://dx.doi.org/10.2174/0929867323999160625124424 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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