Enfuvirtide is a new class of antiviral drug, fusion inhibitors, which interferate with penetration of HIV-1 in the cells. Enfuvirtide exhibits potent and selective inhibition of membrane of viral and cells. It specifically inhibits the function of the gp41 transmembrane glycoprotein of HIV-1. Enfurvitide showed significantly efficacy in the combination with other antiviral drugs in early stadium of HIV infection and in patients with antiretroviral resistention. Local injection site reactions are the most common adverse events associated with enfurvitide. However, the need for subcutaneous application of enfurvitide is a distinct disadvantage, especially in patients who are already burdened by complex oral therapy.