摘要
人类南美洲锥虫病,通常称为美洲锥虫病是世界上最被忽略的疾病之一和拉丁美洲最流行的慢性感染疾病之一并有着每年上千的 新案例。唯一的治疗方案被发现在50年之前。它们具有严重的,不希望的副作用和在该疾病的慢性阶段争议的好处 - 一个特性和衰弱心肌病和/或大型内脏。因此,许多实验研究员在努力找到更好的药物。尽管近年来有许多临床试验,但是他们之间在机制机理方面存在一些差异性,所以药物传递途径发展的结果不乐观。最近的一个失败案例使得易碎性暴露,两个候选药物沙康唑和E1224在二期临床试验中在治疗病人中作用很弱。这样的挫折强调需要连续的,新颖的,高品质的药物发现和开发力度,探索更好,更安全的治疗方法。 在本文中,我们将回顾过去和当前的药物发现的克氏锥虫在过去的半个世纪由学术研究团体,产业界和其他研究机构的研究结果。我们也分析了当前研究的景观,在不久的将来,现在是更好地比以往任何时候都能够提供对南美锥虫病替代疗法。
关键词: 克氏锥虫,美洲锥虫病,苄硝唑,硝呋莫司,药物发现,化学疗法
Current Medicinal Chemistry
Title:Current and Future Chemotherapy for Chagas Disease
Volume: 22 Issue: 37
Author(s): Luís Gaspar, Carolina B. Moraes, Lucio H. Freitas-Junior, Stefania Ferrari, Luca Costantino and Maria Paola Costi, Ross P. Coron, Terry K. Smith, Jair L. Siqueira-Neto, James H. McKerrow and Anabela Cordeiro-da-Silva
Affiliation:
关键词: 克氏锥虫,美洲锥虫病,苄硝唑,硝呋莫司,药物发现,化学疗法
摘要: Human American trypanosomiasis, commonly called Chagas disease, is one of the most neglected illnesses in the world and remains one of the most prevalent chronic infectious diseases of Latin America with thousands of new cases every year. The only treatments available have been introduced five decades ago. They have serious, undesirable side effects and disputed benefits in the chronic stage of the disease – a characteristic and debilitating cardiomyopathy and/or megavisceras. Several laboratories have therefore focused their efforts in finding better drugs. Although recent years have brought new clinical trials, these are few and lack diversity in terms of drug mechanism of action, thus resulting in a weak drug discovery pipeline. This fragility has been recently exposed by the failure of two candidates; posaconazole and E1224, to sterilely cure patients in phase 2 clinical trials. Such setbacks highlight the need for continuous, novel and high quality drug discovery and development efforts to discover better and safer treatments.
In this article we will review past and current findings on drug discovery for Trypanosoma cruzi made by academic research groups, industry and other research organizations over the last half century. We also analyze the current research landscape that is now better placed than ever to deliver alternative treatments for Chagas disease in the near future.
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Luís Gaspar, Carolina B. Moraes, Lucio H. Freitas-Junior, Stefania Ferrari, Luca Costantino and Maria Paola Costi, Ross P. Coron, Terry K. Smith, Jair L. Siqueira-Neto, James H. McKerrow and Anabela Cordeiro-da-Silva , Current and Future Chemotherapy for Chagas Disease, Current Medicinal Chemistry 2015; 22 (37) . https://dx.doi.org/10.2174/0929867322666151015120804
DOI https://dx.doi.org/10.2174/0929867322666151015120804 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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