Artemisinin and its derivatives, in combination with partner drugs, are currently the most effective treatments for malaria parasite infection. Even though artemisinin has been widely used for decades, its mechanism of action had remained controversial until recently. Artemisinin combination therapies (ACTs) have recently been found to be losing efficacy in Southeast Asia. This ‘artemisinin resistance’, defined by a delayed parasite clearance time, has been associated with several genetic mutations. As with any other drug resistance phenotype, resistance can best be understood based on its mechanism of action. Recently, it was demonstrated that artemisinin attacks multiple parasitic targets, suggesting that mutations in drug targets are unlikely to cause high-level artemisinin resistance. These findings will help us to better understand the mechanisms of artemisinin resistance and suggest protocol modifications that may improve the efficacy of ACTs.

青蒿素及其衍生物与伙伴药物联合使用，是目前治疗疟疾寄生虫感染的最有效方法。尽管青蒿素已被广泛使用数十年，但其作用机制直到最近仍存在争议。最近发现青蒿素联合疗法 (ACTs) 在东南亚失去疗效。这种由寄生虫清除时间延迟定义的“青蒿素抗性”与多种基因突变有关。与任何其他耐药性表型一样，可以根据其作用机制最好地理解耐药性。最近，有研究表明青蒿素攻击多个寄生靶点，表明药物靶点的突变不太可能导致高水平的青蒿素耐药。