AUTHOR=Ma Zhaowu , Woon Clariis Yi-Ning , Liu Chen-Guang , Cheng Jun-Ting , You Mingliang , Sethi Gautam , Wong Andrea Li-Ann , Ho Paul Chi-Lui , Zhang Daping , Ong Peishi , Wang Lingzhi , Goh Boon-Cher 

TITLE=Repurposing Artemisinin and its Derivatives as Anticancer Drugs: A Chance or Challenge?

JOURNAL=Frontiers in Pharmacology

VOLUME=Volume 12 - 2021

YEAR=2021

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.828856

DOI=10.3389/fphar.2021.828856

ISSN=1663-9812

ABSTRACT=Cancer has grown to become a global health issue, accounting for one out of six deaths. Despite the recent advances in oncology, there is still an ever-growing need for new therapies that can be made readily accessible. The process of drug discovery and development is arduous and takes many years, and while it is ongoing, the timeframe for lead compounds to reach the point of clinical trials is very long. Drug repurposing has gained traction as it expedites and hastens the process of discovering new entities potentially used for anticancer therapy. One such potential candidate is the antimalarial, artemisinin that has shown to exert anticancer effects in vitro and in vivo. In this review, major molecular and cellular mechanisms of anticancer effect induced by artemisinin and its derivatives have been summarized. Furthermore, major mechanisms of action and some key signalling pathways that this group of compounds work by have been reviewed to explore potential targets which contribute to the proliferation and metastasis of tumour cells. Pharmacokinetic properties, anticancer potency and current formulations that hinder the clinical translation of artemisinin as an anticancer agent, despite its established profile in malaria treatment, are also discussed. Finally, potential solutions or new strategies have been identified to overcome the bottlenecks in repurposing artemisinin‐type compounds as anticancer drugs.