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[被忽视热带病药物研发联盟的活动]

[Activity of NTDs Drug-discovery Research Consortium].

作者信息

Namatame Ichiji

机构信息

Medicinal Chemistry Research Labs. Drug Discovery Research, Astellas Pharma Inc.

出版信息

Yakugaku Zasshi. 2016;136(2):231-6. doi: 10.1248/yakushi.15-00233-4.

Abstract

Neglected tropical diseases (NTDs) are an extremely important issue facing global health care. To improve "access to health" where people are unable to access adequate medical care due to poverty and weak healthcare systems, we have established two consortiums: the NTD drug discovery research consortium, and the pediatric praziquantel consortium. The NTD drug discovery research consortium, which involves six institutions from industry, government, and academia, as well as an international non-profit organization, is committed to developing anti-protozoan active compounds for three NTDs (Leishmaniasis, Chagas disease, and African sleeping sickness). Each participating institute will contribute their efforts to accomplish the following: selection of drug targets based on information technology, and drug discovery by three different approaches (in silico drug discovery, "fragment evolution" which is a unique drug designing method of Astellas Pharma, and phenotypic screening with Astellas' compound library). The consortium has established a brand new database (Integrated Neglected Tropical Disease Database; iNTRODB), and has selected target proteins for the in silico and fragment evolution drug discovery approaches. Thus far, we have identified a number of promising compounds that inhibit the target protein, and we are currently trying to improve the anti-protozoan activity of these compounds. The pediatric praziquantel consortium was founded in July 2012 to develop and register a new praziquantel pediatric formulation for the treatment of schistosomiasis. Astellas Pharma has been a core member in this consortium since its establishment, and has provided expertise and technology in the area of pediatric formulation development and clinical development.

摘要

被忽视的热带病是全球医疗保健面临的一个极其重要的问题。为了改善那些因贫困和医疗体系薄弱而无法获得充分医疗服务地区的“健康可及性”,我们成立了两个联盟:被忽视的热带病药物研发联盟和儿童用吡喹酮联盟。被忽视的热带病药物研发联盟由来自产业界、政府和学术界的六家机构以及一个国际非营利组织组成,致力于开发针对三种被忽视的热带病(利什曼病、恰加斯病和非洲昏睡病)的抗原生动物活性化合物。每个参与机构将共同努力完成以下工作:基于信息技术选择药物靶点,并通过三种不同方法进行药物研发(计算机辅助药物研发、“片段进化”——这是安斯泰来制药独特的药物设计方法,以及使用安斯泰来化合物库进行表型筛选)。该联盟建立了一个全新的数据库(综合被忽视热带病数据库;iNTRODB),并为计算机辅助和片段进化药物研发方法选择了靶蛋白。到目前为止,我们已经鉴定出了许多能够抑制靶蛋白的有前景的化合物,并且我们目前正在努力提高这些化合物的抗原生动物活性。儿童用吡喹酮联盟于2012年7月成立,旨在开发并注册一种用于治疗血吸虫病的新型儿童用吡喹酮制剂。自成立以来,安斯泰来制药一直是该联盟的核心成员,并在儿童制剂开发和临床开发领域提供了专业知识和技术。

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