Nanoparticles have properties that are useful for the diagnosis and treatment of cancer, including their size-dependent properties, stability in solvent, ideal size for delivery within the body, and tunable surface chemistry for targeted delivery. Several different nanoparticle building blocks possessing varied functionality can be assembled into one multifunctional composite nanoparticle, further expanding their potential use in cancer diagnostics and therapeutics. Here, we present several examples of the types of functional composite nanoparticles that have been studied, in addition to highlighted applications of their uses.