Targeted cancer chemotherapy agents interfere with receptor tyrosine kinase signaling pathways that promote tumor cell growth. Targeted agents inhibit receptor tyrosine kinase signaling by binding the extracellular component of a growth receptor, binding the soluble ligand that triggers the receptor, or binding intracellular sites that interfere with downstream signaling events. Since their introduction, targeted agents have proved effective for the treatment of locally advanced, metastatic, and micrometastatic solid tumors. In this article, the targeted agents used for solid malignancies and the evidence for current tumor-specific therapies are reviewed.