Modern medical oncology has introduced various anti-cancer drugs since the World War I and II. Unlike for the solid tumors, hematological malignancies had been documented some limitations for curing it with chemotherapeutic agents only. In 1960, Dr. Nowell and Dr. Hungerford had discovered elongated chromosome (Philadelphia chromosome) which has documented as a product of translocation between 9th and 22nd chromosome in the patients with chronic myeloid leukemia. In 1970s, immunochemistry technique using monoclonal antibody has spread world widely and from 1990s, flow cytometry method has been available. In appreciation of these evolutions in basic science, the treatment strategy ofhematological malignancies has changed from the chemotherapeutic agents to targeted agents. Among the targeted agents, some drugs are newly developed and others are recreated as anti- cancer drugs after long-time of discard because of their toxicities or teratogenic effects. Nowadays, we are in the middle of flood of targeted agents, for example, tyrosinekinase inhibitors, epidermal growth factor receptor blockers, farnesyl transferase inhibitors,histone deacetylase inhibitors, and etc. In 21st century, the optimal treatment of hematological malignancies should follow a tailor- made strategy according to the patient and disease itself. In the present article, some representative agents will be introduced in accordance with target diseases.