Current cancer chemotherapy often suffers severe side-effects of the administered cancer drugs on the normal tissues. In addition, poor bioavailability, due to the low water solubility of the anticancer drugs, limits their applications in chemotherapy. New delivery technologies could help overcome this challenge by improving the water solubility and achieving the targeted delivery of the anticancer drugs. Linear–dendritic hybrid nanomaterials, which combine the highly branched architectures and multifunctionality of dendrimers with the processability of traditional linear–linear block copolymers, have been introduced as ideal carriers in anticancer drug delivery applications. This review presents recent advances in the investigational aspects of linear–dendritic copolymers to be applied as anticancer drug delivery vehicles. We highlight the structures, synthesis of linear–dendritic block copolymers, interaction mechanisms between linear–dendritic copolymers and anticancer drug molecules, and findings on their drug release behavior and anticancer efficacies in vitro and in vivo.