Small-molecule target drugs, as organic compounds with low molecular weight, have a great ease in entering the cell, thus allowing them to target the molecules inside the cell. Several benefits can be derived from small molecules as therapeutic agents, including the ability to be taken orally and their ability to cross cell membranes to reach intracellular locations. The objective of this chapter is to examine whether small molecules can be used to target specific types of cancer at a molecular level. As a result of the insights and perspectives that are presented in this chapter, it is important to note how small molecules will have a major impact on the future approach of targeted cancer therapy. With the progress of our understanding of cancer biology and the advancement of technology, small molecules will have the potential to contribute to better, more personalized treatments for cancer that are less toxic and more effective as our understanding of cancer biology deepens. Toward the advancement of precision medicine in cancer care and improving patient outcomes, the continued research in this field promises to make a significant contribution to the field.