This book discusses the current state of knowledge about potential drug targets against malaria. It reviews the current drug targets and focuses on the progress made on the latest scientific and technological advances in discovering and developing novel antimalarial agents. The initial chapter discusses the existing antimalarial agent, including quinoline derivatives, an antifolate, and artemisinin derivatives. It further explores the potential of Plasmodium kinases as drug targets for the treatment of malaria. Notable, the book examines the major metabolic pathways of the parasite that are explored as novel sites for drug design, including heme detoxification, fatty acid synthesis, nucleic acid synthesis, fatty acid synthesis, and oxidative stress. This volume also presents antineoplastic chemotherapy that targets DNA replication and other cancer agents against the malaria parasites with possible off-target action. Lastly, it discusses Plasmodium proteases, a suitable multistage target for designing novel drugs with new modes of action to combat malaria.