Abstract: There have been exciting advances in the treatment for systemic lupus erythematosus(SLE) with a better understanding of the pathogenesis. Since the long term use of traditional medicines such as glucocorticoids may have negative impacts on the outcome, novel treatments have increasingly specific targets that result in fewer adverse side effects. Medicines newly approved or undergoing clinical trials, such as rituximab, belimumab, anifrolumab, and baricitinib, mainly target at lymphocytes, cytokines, or their intracellular signaling pathways. A combinatory treatment that simultaneously blocks multiple targets may bring better efficacy. Development of the pharmacological treatment is a process evolving from chemical agents to biologics and back to small molecule chemical inhibitors. The modality of treatment is involved in a spiral manner from non-specific to specific and then to the combination of multi-target therapy.