Artemisitene is primarily investigated for its potential antimalarial properties. It shows activity against Plasmodium falciparum, the parasite responsible for the most severe form of malaria. Its mechanism likely involves interference with parasite metabolism through the generation of reactive oxygen species upon interaction with heme or iron, leading to oxidative damage within the parasite. Due to structural similarities with artemisinin, artemisitene is considered a possible contributor to the overall efficacy of Artemisia annua extracts used in traditional and modern antimalarial treatments. Research also explores its role as a biosynthetic intermediate in artemisinin production, which could aid in developing more efficient synthesis methods for artemisinin-based drugs. Limited studies suggest possible anticancer effects, but these remain preliminary and require further validation.