Chirality, a fundamental property of biological systems, is intrinsic to numerous natural biosystems and plays a vital role in sustaining physiological processes. Leveraging their high specificity for biological targets, chiral nanomaterials have emerged as multifunctional tools in cancer therapy. These nanomaterials demonstrate superior biocompatibility, minimal cytotoxicity, and enhanced cellular penetration. Furthermore, the tunability of their surface structures enables precise chirality control, fostering the development of advanced biomaterials capable of targeting tumor metabolism, inducing apoptosis, and modulating immune responses. This review provides a comprehensive overview of recent advancements in the utilization of chiral materials for tumor-targeted therapies, metabolic modulation, apoptotic pathway intervention, photothermal applications, chiral cytotoxic effects, and immunomodulation. Moreover, we elucidate the mechanisms underlying these actions, examine the opportunities and challenges associated with employing chiral materials in oncology, and propose future directions for their advancement. Through the integration of these multifaceted strategies, chiral materials present considerable promise for improving the precision and efficacy of cancer therapeutics.