Cancer is one of the leading causes of mortality and morbidity due to lack of appropriate noninvasive diagnostic and suitable drug delivery system, site-specific accumulation and action of chemotherapeutic drugs as well as enhanced cytotoxicity of normal healthy tissues and cells and cancer-associated multidrug resistance (MDR). The integral development of nanotechnology and nanomedicine has transfigured cancer cure by developing and providing potential methods for targeted drug delivery. Nanoparticles (NPs) and nanomaterials are explored as potential tool for the cancer diagnosis, treatment and management because of their specific properties including biological compatibility, enhanced permeability and retention (EPR) effects and precision for site-specific drug delivery and reduced toxicity. These properties of NPs and nanomaterial overcome several challenges of conventional chemotherapy. Over the years, several nanomaterials such as liposomes, polymeric micelles, dendrimers, carbon nanotubes and quantum dots are widely used for the cancer therapy. Few nanomaterials like nanoshells, gold NPs and quantum dots are explored for diagnostic and well as for chemotherapy. These NPs and nanomaterials successfully eliminate or reduce the problems associated with conventional chemotherapy. This chapter highlighted the different therapeutic strategies including gene therapy, immunotherapy, stimuli-responsive drug release, photothermal therapy (PTT) and photodynamic therapy (PDT) utilizing active NPs and nanomaterials for cancer diagnosis and chemotherapeutic treatment. Additionally, representing a short on future research requirements for providing tailored, efficient and noninvasive treatments.