Tyrosine kinases are important role in cell proliferation & differentiation of cell. Tyrosine kinases involved in diverse biological processes like growth, differentiation, metabolism and apoptosis in response to external and internal stimuli, mediator of signaling cascade. Tyrosine kinases are enzymes that selectively phosphorylates tyrosine residue in different substrates. Over expression of these tyrosine kinases receptor cause development of human cancer. So lot of work is done to understand role of tyrosine kinases in the pathophysiology of cancer. Defective regulation of growth processes plays a role in the genesis and progression of most type of cancer. Oncogenic activation of tyrosine kinase due to mutation, autocrine-paracrine stimulation in cancer cells can be blocked by selective tyrosine kinase inhibitors and thus considered as a promising approach for treatment of cancer. This review describes the role of TK receptors in development of cancer & the role of TK inhibitors on treating cancer. Glivec, Iressa and Terceva most successful tyrosine kinase inhibitor approved by FDA. The revolution in antibody technology allows producing humanized, human chimeric or bispecific monoclonal antibody for targeted cancer therapy. For e. g. Herceptin approved by FDA was first genome based targeted anticancer agent.