Background: Antiretroviral therapy is the cornerstone treatment for people living with human immunodeficiency virus (HIV). Clinical practice guidelines for antiretroviral therapy have been developed.Current Concepts: After the introduction of zidovudine, more than 30 antiretroviral agents have been approved for the treatment of HIV infection. Since a controlled trial proved the efficacy and safety of combination antiretroviral therapy, virologic suppression, immune reconstitution, and long-term survival of people living with HIV have been achievable goals. Early antiretroviral treatment for all people living with HIV is an effective strategy to maintain individual health and prevent the transmission of HIV infection. Selecting an appropriate combination antiretroviral therapy requires careful consideration of various factors, including regimen characteristics, pretreatment viral load and CD4+ cell counts, comorbid conditions, and the anticipated level of compliance. Ongoing advances in antiretroviral treatment, such as the development of long-acting injectables and medications targeting multidrug-resistant HIV, address challenges in the treatment of HIV infection.Discussion and Conclusion: Although cure of HIV infection is impossible with current antiretroviral treatment, HIV infection has become a chronic disease with long-term survival. Hence, clinicians should have knowledge of antiretroviral treatment guidelines.