Hormonal antineoplastic drugs of action is usually considered to function by binding with specific hormone receptors. Hormone receptors, all of which are cytoplasmic protein and nucleoprotein, combined with the hormone with high affinity and specificity. After penetrating the cell membrane and getting into the cells, endogenous or exogenous steroids bind to specific receptors and form the hormone-receptor complexes and activated into the nucleus. The activated hormone receptor complexes, binding to specific receptors of chromatin, react with the role of various components of the nucleus, which causes DNA replication and cell division by a series of enzymatic reactions, thus affecting the physiological function of cells. Adrenocorticotropic hormone, that works on lymphocytes, making it dissolve directly and inhibiting mitosis role, plays an important role in the treatment of lymphoma, leukemia and multiple myeloma. It should be attached care in the use of hormone to treat related tumors, and the hormone must be selected carefully by theoretical basis, in line with the indications, and with dosage properly, otherwise it will promote the growth of tumor cells, just the opposite. This antineoplastic drugs include aromatase inhibitors, aromatase inactivator, estrogens, anti-estrogens, progestins, androgens, anti-androgens, luteinizing hormone agonists, glucocorticoids hormones, adrenal blockers and others.