Advances in solid tumor treatment have been enormous in the past decade, especially molecularly targeted therapy, for which aberrant molecules or biological pathways relating to tumor growth and development have been targeted specifically. Molecularly targeted therapy agents show activity against specific tumor cells with little effect on normal vital organs or tissues, making them a more tolerable therapeutic approach for patients than chemotherapeutic agents. Tyrosine kinase receptor inhibitors are molecularly targeted therapeutic agents that inhibit signal transduction pathways. To date, a number of agents in this category have been approved for solid cancer treatment such as in lung, breast, and colon cancers. This review highlights the role of the approved tyrosine kinase receptor inhibitors for solid tumor therapy.