Medicines for Malaria Venture, 20 route de Pre-Bois, 1215 Geneva, Switzerland.
Medicines for Malaria Venture, 20 route de Pre-Bois, 1215 Geneva, Switzerland.
Curr Opin Pharmacol. 2018 Oct;42:1-6. doi: 10.1016/j.coph.2018.05.006. Epub 2018 May 31.
Over the past decade, new high-throughput phenotypic assays with malaria parasites have been developed, and these were used to screen millions of compounds. This effort, as well as improving older chemical scaffolds and optimising compounds against both known and new drug targets has resulted in the discovery of exciting new pipeline drug candidates that are now being evaluated in a number of clinical trials. In addition, the pitfalls and opportunities from this experience has led to a better definition of the optimal target compound and product profiles for new antimalarials, including medicines that treat uncomplicated or severe malaria, provide chemoprevention, or stop disease transmission, covering all stages of the parasite. An important decision element is how to combine these new molecules with existing ones in today's dynamic resistance landscape.
在过去的十年中，已经开发出了新的高通量疟原虫表型测定方法，并利用这些方法对数百万种化合物进行了筛选。这项工作，以及改进旧的化学结构和针对已知和新的药物靶点优化化合物的工作，已经发现了令人兴奋的新的候选药物，这些药物现在正在一些临床试验中进行评估。此外，从这些经验中吸取的教训和机会，导致对新抗疟药物的最佳目标化合物和产品特征有了更好的定义，包括治疗轻症或重症疟疾、提供化学预防或阻止疾病传播的药物，涵盖寄生虫的所有阶段。一个重要的决策因素是如何在当今充满活力的耐药性环境中结合这些新分子和现有的药物。
