This review discusses receptor-targeted nanomedicine for cancer therapy, focusing on overexpressed receptors on tumor cells and various nanocarrier systems used for targeted drug delivery. It highlights therapeutic modalities such as small molecules, aptamers, peptides, antibodies, and cell-based strategies, emphasizing clinical developments and challenges in translating nanocarrier-based targeting strategies into clinical practice. The article also outlines future directions for improving cancer-targeted therapy to enhance treatment efficacy while minimizing toxicity. Key receptors discussed include the Epidermal Growth Factor Receptor (EGFR), Folate Receptor, Transferrin Receptor, Integrins, Mucin-1 (MUC1), CD44, Hormone Receptors, and Programmed Death-1 (PD-1) Receptor. Each receptor's role in cancer development, signaling pathways, and potential as a therapeutic target are explored. The review also covers various nanocarrier types, including lipid-based systems like liposomes, solid lipid nanoparticles (SLNs), phytosomes, and nanostructured lipid carriers (NLCs), as well as polymeric systems such as dendrimers. These nanocarriers are designed to improve drug delivery, targeting, and therapeutic outcomes in cancer treatment. The review underscores the importance of understanding receptor biology and nanocarrier interactions to develop effective, clinically translatable cancer therapies.This review discusses receptor-targeted nanomedicine for cancer therapy, focusing on overexpressed receptors on tumor cells and various nanocarrier systems used for targeted drug delivery. It highlights therapeutic modalities such as small molecules, aptamers, peptides, antibodies, and cell-based strategies, emphasizing clinical developments and challenges in translating nanocarrier-based targeting strategies into clinical practice. The article also outlines future directions for improving cancer-targeted therapy to enhance treatment efficacy while minimizing toxicity. Key receptors discussed include the Epidermal Growth Factor Receptor (EGFR), Folate Receptor, Transferrin Receptor, Integrins, Mucin-1 (MUC1), CD44, Hormone Receptors, and Programmed Death-1 (PD-1) Receptor. Each receptor's role in cancer development, signaling pathways, and potential as a therapeutic target are explored. The review also covers various nanocarrier types, including lipid-based systems like liposomes, solid lipid nanoparticles (SLNs), phytosomes, and nanostructured lipid carriers (NLCs), as well as polymeric systems such as dendrimers. These nanocarriers are designed to improve drug delivery, targeting, and therapeutic outcomes in cancer treatment. The review underscores the importance of understanding receptor biology and nanocarrier interactions to develop effective, clinically translatable cancer therapies.