Malaria is a major tropical disease where important needs are to mitigate symptoms and to prevent the establishment of infection. Cyclopeptides containing <i>N</i>-methyl amino acids with <i>in vitro</i> activity against erythrocytic forms as well as liver stage are presented. The synthesis, parasitological characterization, physicochemical properties, <i>in vivo</i> evaluation, and mice pharmacokinetics are described.