The HIV (human immunodeficiency virus) entry process, the first step of the HIV replication cycle, plays a significant role in the subsequent viral infections and human immune system collapse. Virus binding and entrance into the host cell involves multiple steps, including viral attachment, co-receptor interactions, and membrane fusion. This sequence of events offers several potential targets for therapeutic interference. Some antiretroviral drugs that interact with different targets involved in the entry process have been tested in various phases, but only two of them were approved for clinical application. This study attempts to provide an overall research and development (R&D) landscape of HIV entry inhibitors by reviewing relevant projects (78 projects were collected for this study). The entry inhibitors have been divided into three classes based on their functional targets: attachment inhibitors, co-receptor inhibitors, and fusion inhibitors. The development profiles are integrated to provide a clinical overview of entry inhibitors. Furthermore, the performance of each class of inhibitor in clinical trials is summarized to demonstrate their specific roles in anti-HIV therapy.