Integrase inhibitors and CCR5 receptor antagonists, novel class of antiretrovirals, were introduced into clinical practice in late 2000s. Currently available drugs in these classes, raltegravir and maraviroc, show good tolerability and have little impact on lipid or glucose metabolism compared to traditional classes. Disadvantage of these two drugs is the need for twice-daily dosing. The usefulness of raltegravir in both treatment-naïve and treatment-experienced setting has been well established through clinical trials and five years' clinical use, whereas the usefulness of maraviroc in treatment-naïve setting is still unclear. These drugs will be utilized as a key component of NRTI-sparing regimens in the future.