Malaria continues to be a major public health concern in many tropical and subtropical regions, causing significant morbidity and mortality worldwide. Despite ongoing control measures, the emergence of drug-resistant Plasmodium species has complicated treatment strategies, creating an urgent need for novel therapeutic approaches. Recent research has explored innovative antimalarial agents, combination therapies, and targeted drug delivery systems to enhance treatment efficacy and overcome resistance. This review summarizes recent advancements in antimalarial drug development, focusing on new molecular targets, improved formulations, and combination regimens. The discussion also highlights the importance of integrating modern drug discovery techniques, such as structure-based design and high-throughput screening, to accelerate the development of effective, safe, and affordable antimalarial medicines.