Cancer remains one of the leading causes of mortality worldwide, and conventional treatment strategies such as surgery, radiotherapy, and chemotherapy are often limited by tumor recurrence and adverse side effects. In recent years, nanotechnology-based targeted therapies have emerged as promising strategies to improve therapeutic specificity and reduce systemic toxicity. Among these approaches, elastin-like polypeptides (ELPs), a class of synthetic thermoresponsive biopolymers composed of repetitive peptide sequences, have attracted considerable attention for biomedical applications. ELPs exhibit several advantageous properties, including inverse transition temperature behavior, high biocompatibility, biodegradability, self-assembly capability, and structural stability. This review discusses the structural characteristics, de novo synthesis, and purification methods of ELPs. Furthermore, it highlights recent advances in the use of ELP-conjugated anticancer agents, including chemotherapeutic drugs, small molecules, peptides, and proteins, for targeted drug delivery in cancer therapy. Additionally, this article addresses the challenges associated with the use of these nanoparticles as drug delivery systems and compares them with other biomaterials. These emerging ELP-based platforms offer significant potential for the development of innovative and effective therapeutic strategies against various types of cancer.