Lumefantrine and trimethoprim are antimalarial and antibiotic drugs respectively. Even though, therapeutic agents have shown enhanced efficacy upon coordination to metal ion, antimalarial activity of lumefantrine-trimethoprim-copper complex drug has not been reported. This study evaluated the anti-malarial potency and safety of synthesized lumefantrinetrimethoprim-copper (LTC) complex in mice. A total of 35 albino mice were randomly divided into seven groups. Mice in groups 1 and 7 were not infected with Plasmodium berghei. Infected mice in groups 3, 4, 5, and 6 were treated with chloroquine, LTC, trimethoprim and lumefantrine respectively. All the animals were sacrificed 24 hours after completion of their doses. Percentage parasitaemia, chemo suppression attained in the group of mice infected, but treated with LTC (96.84%) or chloroquine (97.80%) was higher than those treated with lumefantrine (75.79%) or trimethoprim (76.84%) at day 8 post-inoculation, when compared with control. There was significant reduction in the activities of ALP, ALT and AST in the liver of treated mice when compared with control. Increased chromosomal aberration was observed in all treated groups when compared with control.The observed modifications in the biochemical indices and the presence of chromosomal aberrations in the organs studied, suggested a selective and functional toxicity of the drug.