Abstract: Lymphoma is a group of heterogeneous hematological malignant tumors originating from lymph nodes or other lymphoid tissues, including Hodgkin's lymphoma and non-Hodgkin's lymphoma. Diffuse large B-cell lymphoma (DLBCL) is one of the most common subtypes of non-Hodgkin's lymphoma (NHL) with obvious heterogeneity. Standard R-CHOP regimen (rituximab combined with cyclophosphamide, adriamycin, vincristine and prednisone) can significantly improve the survival of more than 60% of patients. However, there are still about 30% - 40% of patients with relapse or refractory disease, and the prognosis is very poor. How to prolong the survival of relapsed/refractory DLBCL patients and improve their prognosis has become a research hotspot. With the continuous in-depth study of gene expression profiles and molecular mechanisms of drug resistance, new chemotherapy schemes and new drugs emerge, which brings new hope for individualized precise treatment of relapsed/refractory DLBCL. This article reviews the recent progress of targeted drugs in the treatment of relapsed/refractory DLBCL.