Artemether is a semisynthetic derivative of artemisinin, a phytoconstituent that acts as a short-acting antimalarial agent and is used to treat uncomplicated Plasmodium falciparum malaria. Artemisinin derivatives kill parasites more rapidly than conventional antimalarial drugs, and are active against both the sexual and asexual stages of the parasite cycle. However due to their short half-life (and to prevent resistance development) artemisinin compounds are often combined with long-acting antimalarial drugs. Artemeter is administered orally and as an oil-based intramuscular injection. The antimalarial activity of artemether and other artemisinin derivatives is a result of the peroxide bridge found in the active metabolite dihydroartemisinin. Dihydroartemisinin is formed from the rapid demethylation of artmether via CYP3A4 and CYP3A5. It then undergoes glucuronidation catalyzed by the UDP-glucuronosyltransferases UGT1A9 and UGT2B7 into inactive metabolites that are eliminated in the bile.

Artemether Pathway References