Advances in the development of HIV integrase strand transfer inhibitors

HIV-1 integrase (IN) is a key enzyme in viral replication that catalyzes the covalent integration of viral cDNA into the host genome. Currently, five HIV-1 IN strand transfer inhibitors (INSTIs) are approved for clinical use. These drugs represent an important addition to the armamentarium for antiretroviral therapy. This review briefly illustrates the development history of INSTIs. The characteristics of the currently approved INSTIs, as well as their future perspectives, are critically discussed. • HIV-1 integrase is an essential enzyme for retroviral replication. • This review is focused on the development history of INSTIs. • The characteristics of the FDA approved INSTIs are depicted.