The treatment of malaria has significantly improved with the groundbreaking antimalarial drug artemisinin, which is derived from Artemisia annua. It was found in the 1970s and damages Plasmodium parasites by producing reactive oxygen species. Because of its quick action and effectiveness against drug-resistant strains, artemisinin-based combination treatments (ACTs) are the gold standard. However, long-term efficacy is threatened by resistance, particularly in Southeast Asia. The history, mechanism, and clinical application of artemisinin are examined in this chapter, along with its function in the prevention of malaria and current studies aimed at overcoming resistance and creating novel derivatives. In the worldwide battle against malaria, artemisinin is still essential.