Integrase inhibitors work by inhibiting the enzyme integrase, which is responsible for integration of viral DNA into the DNA of the infected cell.

Integrase inhibitors are used in combination with other antiretroviral medications for the treatment of HIV to prevent the virus from spreading in the body and to reduce the amount of virus in the bloodstream.

In 2007, the FDA approved raltegravir (Isentress) for use in individuals whose infection has proven resistant to other HAART drugs.