Although immune suppressive drugs have contributed for the cancer chemotherapy, organ transplant, but their therapeutic efficacy is limited. This study aims to evaluate the immunological modulations induced by four representative immunosuppressive on THP-1 cell line. 75% cell viabilities were determined and four test concentrations, 0.01X, 0.1X, 0.5X, and vehicle control were chosen. Culture supernatants were collected at 24 h after lipopolysaccharide (LPS1 ㎍/㎖) activation in the presence of test substances. 27 target cytokines were measured through luminex system and relative cytokine production levels (RCPLs,%) were calculated. Cytokines with the RCPL below 100% at all the three concentrations were 21 including IL-1beta, -1ra, -2, -4, -5, -6, -7, -9, -10, -12, -13, -15, -17, Eotaxin, FGF-basic, GM-CSF, IFNγ, IP-10, MCP-1α, PDGF-BB, and VEGF in dexamethasone-treated cells. Concerning on cyclophosphamide, the RCPLs on 11 cytokines were less than 100% at all the 3 concentrations. Treatment of cyclosporine demonstrated 10 cytokines with below 100% RCPL at all the 3 concentrations. The RCPLs below 100% were observed with 22 cytokines including IL-1β, -1ra, -2, -4, -5, -6, -7, -9, -12, -13, -15, -17, Eotaxin, GFG-basic, G-CSF, GM-CSF, IFNγ, MCP-1, MIP-1α, PDGF-BB, TNFα, a nd VEGF from THP-1 cells t reated w ith tacrolimus a t all the 3 concentrations. The present study indicates that tacrolimus and dexamethasone are stronger immunosuppressants than cyclophosphamide and cyclosporine on THP-1 cell line.