Materials at nano dimensions exhibit totally different properties compared to their bulk and atomic states. This feature has been harnessed by scientists from various disciplines, to develop functional nanomaterials for cancer diagnosis and therapeutics. The success stories range from delivering chemotherapeutic molecules in nano-sized formulations to functional nanomaterials, which deliver thermal and radiotherapy at specific targeted sites. This brief review summarizes the recent developments of various nanotechnologies in cancer therapy and diagnostics, both from the research sector and the upcoming products in pipeline on its route to commercialization. Supportive engineering innovations and frontiers in nanomolecular research, with a potential to revolutionize cancer therapy, have been discussed in brief.