Conventional cancer therapies have some challenges including the broad effects on normal cells, the lack of specificity of radiotherapy, and the emergence of drug resistance. Given these challenges, there is a growing need for anticancer approaches that selectively target malignant cells. Lectin-based targeted drug delivery systems offer a promising solution by providing a more precise and tailored approach to treatment. Lectin-mediated drug targeting operates through the recognition of glycosylated molecules present on the surface of cancer cells, which differ from those on normal cells due to malignant transformation. In this process, lectins function as bioadhesive molecules to target cancer cells. In pathological conditions like cancer, cells exhibit unique glycan patterns compared to healthy cells, making lectins attractive carriers for targeted drug delivery. Specific lectins, sourced from nature or produced through recombinant DNA technology, can be coupled with macromolecular drugs or specialized carriers. This approach enables efficient cellular uptake and intracellular delivery of drugs to specific cells and tissues. The chapter will explore lectins’ specific interactions with cancer cell targets and their potential application in targeted drug delivery systems.