In vitro and in vivo studies of artemisinin endoperoxides

TL;DRAbstract

Artemisinin and its semi-synthetic derivatives (eg. Artemether/ARM, artesunate/ARS, dihydroartemisinin/DHA) play an important role in combating malaria, and treatments containing an artemisinin derivative (artemisinin-based combination therapies, ACTs) are today the standard treatment worldwide for Plasmodium falciparum malaria. In addition to their antimalarial effect, artemisinin endoperoxides have been demonstrated to exert cytotoxic effects, making them interesting candidates for oncologic indications.\nThis thesis specifically aimed to (1) investigate in vitro effects of artemisinin endoperoxides on human liver Cytochrome P450 (CYP) enzyme activity, and to (2) study the pharmacokinetics of ARS and DHA in plasma and saliva during long-term oral ARS treatment in patients with breast cancer. In vitro experimental assays using recombinant and microsomal CYP enzymes were conducted to assess potential inhibitory effects of artemisinin, ARM, ARS and DHA (Papers I and II). Results were ex

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