© 2018 Society of Pharmaceutical Sciences of Ankara (FABAD). All rights reserved.Human immunodeficiency virus (HIV-1) is spreading as an epidemic in Africa and America in the last thirty years. Many drugs have been developed against HIV-1 they are now highly used; however as the virus can modify itself, there is high possibility that it can gain resistance or cross-resistance. Therefore, developing new drugs is essential to prevent this epidemic. In addition, the side effects of the drugs on the market are high and increased efficacy can be achieved by combined therapies. In order to enter the host cell, HIV-1 must attach to CD4 receptors and coreceptors which are on the plasma membrane. Virus cannot enter the cell by only binding to CD4 receptors. The coreceptors are actually chemokine receptors "CCR5" and "CXCR4". Some drug candidates in one of the newly developed drug group "Entry Inhibitors" act as antagonists and they prevent the entry of the virus to host cell by binding to these receptors. However, due to the serious toxic effects of these drug candidates, their marketing will take a long period of time. Today, there is only one entry inhibitor being used, named "Maraviroc". This drug is a CCR5 receptor antagonist that has potent in vivo anti-HIV activity. The results of studies performed on healthy volunteers showed that this substance was safe and had high tolerability. On the other hand, studies on new CCR5 and CXCR4 antagonists in HIV-1 therapy are still going on. In the near future, there is hope that new entry inhibitors with high efficacy and lower side effects will be synthesized. This review will mainly focus on the structure of HIV-1 virus, HIV-1 drugs on the market, HIV-1 entry inhibitors and newly developed coreceptor antagonists and their toxicities.