This review discusses the use of receptor-targeted nanomedicine for cancer therapy, focusing on overexpressed receptors on tumor cells and the potential of nanocarrier systems to target these receptors. It highlights various types of nanocarrier systems and targeting ligands, including small molecules, aptamers, peptides, antibodies, and cell-based targeting strategies. The article covers therapeutic modalities and clinical advancements, while also addressing challenges in the clinical translation of nanocarrier-based targeting strategies. Future directions aim to improve the efficacy of cancer-targeted therapy while minimizing toxicity. The review emphasizes the importance of understanding the roles of key receptors in cancer biology, such as EGFR, folate receptors, transferrin receptors, integrins, MUC1, CD44, hormone receptors, and PD-1, to develop more effective and personalized treatments. Additionally, it details common nanocarrier types, including liposomes, solid lipid nanoparticles (SLNs), phytosomes, nanostructured lipid carriers (NLCs), dendrimers, and polymeric micelles, and their applications in cancer therapy.This review discusses the use of receptor-targeted nanomedicine for cancer therapy, focusing on overexpressed receptors on tumor cells and the potential of nanocarrier systems to target these receptors. It highlights various types of nanocarrier systems and targeting ligands, including small molecules, aptamers, peptides, antibodies, and cell-based targeting strategies. The article covers therapeutic modalities and clinical advancements, while also addressing challenges in the clinical translation of nanocarrier-based targeting strategies. Future directions aim to improve the efficacy of cancer-targeted therapy while minimizing toxicity. The review emphasizes the importance of understanding the roles of key receptors in cancer biology, such as EGFR, folate receptors, transferrin receptors, integrins, MUC1, CD44, hormone receptors, and PD-1, to develop more effective and personalized treatments. Additionally, it details common nanocarrier types, including liposomes, solid lipid nanoparticles (SLNs), phytosomes, nanostructured lipid carriers (NLCs), dendrimers, and polymeric micelles, and their applications in cancer therapy.