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This chapter focuses on the potential of hybrid nanoparticles (NPs) for diagnostics and treatment various disorders, with an emphasis on cancer. The concept of “hybrid NPs” implies to coupling inorganic and organic materials with different physical, chemical, and biological properties to achieve the synergetic effect. It allows an optimization and increasing therapeutic efficacy of original components. The chapter describes the principles and methods of fabrication of hybrid NPs. It also demonstrates how organic and inorganic materials could be combined without sacrificing their biocompatibility and effectiveness. This chapter summarizes and analyzes recent research and progress on novel classes of hybrid NPs. The last part of this chapter is dedicated to future of hybrid NPs and possible clinical applications.