Integrating nanomaterials and biomedicine is a recent endeavor that aims to provide highly localized detection and treatment for cancers and diseases. Understanding the intricate interplay of nanomaterials and biological components and biological systems necessitates combining materials science, nanotechnology, physics, chemistry, biology, and biomedicine. The impact of this grand exploration touches areas of fundamental science and engineering, health care, and environmental control and protection. Recent advances in our understanding of carcinogenesis have led us to consider taking advantage of the special characteristics of both cancer cells and nanomaterials to detect and treat tumors. Integrating cancer therapy and nanomaterials captivates scientific imagination, offers new hope for human well-being, and unavoidably invites controversy and debate as experienced by many scientific and technological developments during their infancy.