Department of Chemistry and Technologies of Drug, Sapienza University of Rome, Rome, Italy.
Expert Opin Ther Pat. 2022 Jun;32(6):649-666. doi: 10.1080/13543776.2022.2049239. Epub 2022 Mar 11.
Despite substantial progress in the field, malaria remains a global health issue and currently available control strategies are not sufficient to achieve eradication. Agents able to prevent transmission are likely to have a strong impact on malaria control and have been prioritized as a primary objective to reduce the number of secondary infections. Therefore, there is an increased interest in finding novel drugs targeting sexual stages of and innovative methods to target malaria transmission from host to vector, and vice versa.
This review covers innovative transmission-blocking inventions patented between 2015 and October 2021. The focus is on chemical interventions, which could be used as 'chemical vaccines' to prevent transmission (small molecules, carbohydrates, and polypeptides).
Even though the development of novel strategies to block transmission still requires fundamental additional research and a deeper understanding of parasite sexual stages biology, the research in this field has significantly accelerated. Among innovative inventions patented over the last 6 years, the surface-delivery of antimalarial drugs to kill transmission-stages parasites in mosquitoes holds the highest promise for success in malaria control strategies, opening completely new scenarios in malaria transmission-blocking drug discovery.
尽管该领域取得了重大进展,但疟疾仍是一个全球性的健康问题,目前可用的控制策略还不足以实现根除。能够预防传播的药物很可能对疟疾控制产生重大影响,并被优先作为减少二次感染数量的主要目标。因此,人们越来越有兴趣寻找针对 和创新方法来针对疟疾从宿主到媒介的传播,反之亦然。
本文综述了 2015 年至 2021 年 10 月期间获得专利的创新型阻断传播发明。重点是化学干预措施,这些措施可用作“化学疫苗”来预防传播(小分子、碳水化合物和多肽)。
尽管开发新型传播阻断策略仍然需要进行基础的额外研究和对寄生虫有性阶段生物学的更深入了解,但该领域的研究已经大大加速。在过去 6 年获得专利的创新发明中,将抗疟药物递送至蚊子以杀死传播阶段寄生虫的表面给药在疟疾控制策略中最有成功的希望,为疟疾传播阻断药物发现开辟了全新的前景。