Abstract: HIV-infected patients need life-long antiretroviral therapy. The most commonly used anti-HIV drugs in China include efavirenz, tenofovir, nevirapine, lamivudine, zidovudine, and lopinavir/ritonavir. In order to explore the pharmacokinetics/pharmacodynamics(PK/PD) profiles of domestic generic antiretroviral drugs and further optimize the therapeutic regimens, researchers conducted a series of PK/PD studies in Chinese HIV-infected patients. The study results indicated that the PK parameters and safety profiles were quite different from those in foreign populations, mainly with higher Cmax and AUC, lower Cl/F and higher incidence of some adverse reactions including hepatotoxicity, rash, bone and renal toxicities, which may be related with body weight and pharmacogenetic factors, suggesting that we may need to adjust the dosing regimens according to the PK/PD profiles in Chinese population. In this article, the PK/PD data of five commonly used antiretroviral drugs in Chinese HIV-infected patients are summarized, aiming to provide reference for optimizing the clinical use of antiretroviral drugs.