Molecular-targeted therapy is a newly developed approach for cancer therapy. With the advantages of lower side effects and higher performance, this approach has become a critical focus of cancer research. There are various molecules that can be treated as therapeutic targets for cancer. These molecules are located in different compartments of cancer cells, such as the cell membrane, cytoplasm, nuclei, and extracellular matrix. In this review, we mainly discussed the current progress in molecular-targeted therapy for cancers and the development of new drugs in this field.