Lumefantrine

Lumefantrine (CAS No.: 82186-77-4) is a synthetic, orally active antimalarial small molecule widely utilized in biomedical research and drug discovery focused on parasitic diseases, particularly Plasmodium falciparum infection. It functions primarily by disrupting the heme detoxification pathway during the intraerythrocytic stage of parasite development, leading to the accumulation of toxic heme species and inhibition of parasite proliferation. Lumefantrine is most commonly studied in combination with artemether as part of artemisinin-based combination therapy, where the complementary mechanisms enhance antimalarial efficacy and reduce the emergence of drug resistance, making it a key component in first- and second-line treatment strategies globally. In addition to its antiparasitic activity, lumefantrine has been reported to inhibit the rapidly activating delayed-rectifier potassium channel (IKr) at low micromolar levels, indicating potential off-target electrophysiological effects relevant to safety pharmacology. In vitro studies typically demonstrate activity in the nanomolar to low micromolar range against malaria parasites, supporting its utility in screening assays and mechanistic studies. In research settings, lumefantrine is applied in cell-based parasite culture systems and in vivo malaria models to investigate drug resistance, combination therapies, and pharmacodynamic interactions, with experimental concentrations or dosing regimens varying according to specific study designs and objectives.