Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 uM. Gardiquimod diTFA could function as both an immune system modifier and a reverse transcriptase inhibitor as a novel therapeutic agent to block systemic and mucosal transmission of HIV-1.(1) (2).