Nanoscale metal-organic frameworks (NMOFs) are hybrid nanomaterials containing organic ligands and inorganic metal ions. In the medical field, NMOFs have demonstrated the ability to transport therapeutic and imaging agents due to their large surface area, porosity, tunable size, and other properties. The versatile components of NMOFs allow the synthesis of a variety of nanostructures with different functions, and their surface can be modified to enhance their biocompatibility and functionality. In addition, NMOFs can be decorated with targeted biomolecules to achieve targeting of tumors or specific organs of interest. This chapter describes and discusses recent advances in NMOFs, particularly for cancer diagnosis and treatment. It highlights the specific properties required for these biomedical applications, including their broad potential as drug delivery systems. Different therapeutic modalities including photodynamic, immunotherapy, and radiotherapy are reviewed. Radiolabeled NMOFs have the potential to be used as nanoplatforms for the precise delivery of combined tumor therapies. Finally, this chapter presents the potential use and future perspectives of NMOFs as theranostic platforms, combining their unique characteristics and advantages as nanosystems.