The prognosis of acute leukemia has been greatly improved by the emergence of new chemotherapeutic agents, intense multi-drug combination chemotherapy and hematopoietic stem cell transplantation, but there is still a lack of effective treatment for refractory and relapsed cases, and adverse effects during treatment are an urgent problem. Targeted therapies proposed for leukemic cell proliferation have recently become an important area of therapeutic research. For example, (1) targeted therapy of monoclonal antibodies, we applied CD33 antibody and induced relapsed leukemia successfully, especially acute promyelocytic leukemia fusion gene relapse, applied CD33 antibody to relieve, and then did autologous hematopoietic stem cell transplantation, the patient was cured and now has survived disease free; (2) targeted therapy of fusion gene; (3) targeted therapy of apoptosis regulators; (4) STAT (4) targeted therapy of signal transduction pathway, the most successful is chronic granulocytic leukemia, foreign reports of positive efficacy, there is a theoretical basis; (5) targeted therapy of DNA methylation, some leukemia and MDS are methylation caused by the disease, elderly leukemia demethylation with decitabine, greatly improve the prognosis of patients; (6) cytokine-receptor-mediated targeted therapy. So targeted therapy opens up new approaches in leukemia.