Translational oncology aims to translate laboratory research into new anticancer therapies. Contrary to conventional surgery, chemotherapy, and radiotherapy, targeted anticancer therapy (TAT) refers to systemic administration of drugs with particular mechanisms that specifically act on well-defined targets or biologic pathways that, when activated or inactivated, may cause regression or destruction of the malignant process, meanwhile with minimized adverse effects on healthy tissues. In this article, we intend to first give a brief review on various known TAT approaches that are deemed promising for clinical applications in the current trend of personalized medicine, and then we will introduce our newly developed approach namely small molecular sequential dual targeting theragnostic strategy as a generalized class of TAT for the management of most solid malignancies, which, after optimization, is expected to help improve overall cancer treatability and curability.