Since the declaration of war on cancer more than 40 years ago, progresses on cancer treatment outcomes have been slow and limited for most part, despite major investments in research and development.However, the realization that cancer is an extremely complex and heterogeneous mixture of diseases, coupled with technological advances in cancer genomics, proteomics, and metabolomics, has led to the development of novel and more effective treatment approaches in recent years.In fact, the approvals of multiple new classes of targeted therapies, particularly anti-cancer immune therapy agents in recent months,may have signaled the arrival of a new era in our fights with cancer.With the expansion of anti-cancer therapeutics toolbox, it is now possible to design individualized treatments to match the genetic makeups of the patients and their tumors.It is fair to say that there is no better time than now for cancer research.This special issue showcases 11 up-to-date reviews written by experts in their corresponding fields covering the major forefronts of targeted cancer drug discovery research.