Objective To investigate the in vitro anti-HIV-1 activity of statins and to evaluate the antiviral of pitavastatin in combination with other anti-HIV drugs. Methods The cytotoxicity of statins on C8166 cells was determined using the MTT assay. The inhibitory effect of statins on HIV-1IIIB-induced cytopathic effect was measured by counting the number of syncytia. The inhibitory effect of statins on the viral replication in C8166 cells acutely infected with laboratory-adapted strains HIV-1IIIB was detected by ELISA. The combination of pitavastatin and anti-HIV drugs with the different targets was measured by ELISA. Results Among statins, pivastatin has significant anti-HIV-1 activity in vitro. The combination of pivastatin with nucleoside reverse transcriptase inhibitors(tenofovir, emtricitabine, lamivudine and zidovudine) and protease inhibitors(indinavir and darunavir) showed synergistic effect. The combination of pivastatin with non-nucleoside reverse transcriptase inhibitor(etravirine) showed antagonism effect. The combination of pivastatin with integrase strand transfer inhibitors(raltegravir and dolutegravir) showed additive effect. Conclusion Pitavastatin showed synergistic or additive effects when combined with other anti-HIV drugs, except for antagonism when combined with etravirine.