The battle between human and the Human immunodeficiency virus (HIV) is on, with both of them rapidly improving their attacking and defense strategies. Many therapeutic agents for HIV infection have been designed and developed, However there are various aspects, like novel targets against HIV, which are yet to be unfolded with a goal of designing and developing novel drug molecules against HIV. This article reviews the current status and innovative new options for antiretroviral therapy for HIV and also discusses the various mechanisms of action for each class of drugs, and the problems yet to be solved with respect to HIV as a target for improvised treatment against AIDS.