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抗疟药物:专利中有哪些新进展?

Antimalarial drugs: what's new in the patents?

机构信息

Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Lisboa, Portugal.

Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Siena, Italy.

出版信息

Expert Opin Ther Pat. 2023 Mar;33(3):151-168. doi: 10.1080/13543776.2023.2203814. Epub 2023 Apr 20.

Abstract

INTRODUCTION

The efficacy of current therapeutic warheads in preventing malaria transmission or treating the disease is often hampered by the emergence of drug-resistance. No effective vaccines are available to date, and novel drugs able to counteract drug-resistant forms of malaria and/or to target multiple stages of the parasite's lifecycle are urgently needed.

AREAS COVERED

This review covers patents that protect antimalarial small molecules bearing the artemisinin or other chemical scaffolds, as well as vaccines, that have been published in the period 2015-2022. Literature was searched in public databases of articles and patents. Patents protecting small molecules that prevent malaria transmission are not discussed herein.

EXPERT OPINION

Significant progress has been made in the design of antimalarial agents. Most of these candidates have been tested in standardized strains, with the use of clinical isolates for testing still underdeveloped. Several compounds have been profiled in mouse models of malaria, including humanized mice. Despite having different efficacy, these new molecules might further progress the field and hopefully will advance to clinical development soon.

摘要

简介

当前的治疗弹头在预防疟疾传播或治疗疾病方面的疗效往往受到耐药性出现的阻碍。迄今为止,尚无有效的疫苗,急需能够对抗耐药性疟疾形式和/或针对寄生虫生命周期多个阶段的新型药物。

涵盖领域

本综述涵盖了 2015 年至 2022 年期间发表的、具有青蒿素或其他化学骨架的抗疟小分子药物和疫苗的专利。文献检索于文章和专利的公共数据库中。本文未讨论可预防疟疾传播的小分子药物的专利。

专家意见

在抗疟药物的设计方面取得了重大进展。这些候选药物大多数都已经在标准化菌株中进行了测试,而使用临床分离株进行测试的方法仍在开发中。一些化合物已在疟疾的小鼠模型中进行了分析,包括人源化小鼠。尽管疗效不同,但这些新分子可能会进一步推动该领域的发展,并有望很快进入临床开发。

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