Abstract: Acquired immune deficiency syndrome (AIDS) is a global epidemic infectious disease caused by infection of human immunodeficiency virus (HIV). Antiretroviral therapy (ART) has achieved significant clinical efficacy and success. However, due to the inability to completely eradicate HIV virus, long-term antiviral therapy may be challenged by toxic and side effects of drugs, emergence of drug-resistant viruses, poor patients' compliance, and inconvenience of daily oral administration. Since vaccines and cures are currently unavailable, there is a continuous demand for new drugs and new strategies against AIDS with the rapid expansion of treatment population as well as significant prolongation of life expectancy and treatment duration. Single-pill combinations, long-acting injectables, broadly neutralizing antibody-mediated immunotherapies, drugs with novel mechanisms of action, and preventive vaccines will play key roles in breaking the bottleneck for prevention and control of AIDS. The advances in antiretroviral therapy and drug development for AIDS have been reviewed in this paper.