We are at the dawn of an era when epigenetic drugs will be an important weapon in our arsenal in the war against cancer. Hematological malignancies have provided a promising starting point, but studies will surely extend to all solid tumors. However, we need to continue our research to develop more specific DNA-demethylating agents, to understand their biologic effects, and to determine whether they may be successfully combined with other epigenetic drugs, such as the inhibitors of histone deacetylases, and classic chemotherapy compounds.