Antiretroviral therapies (ART) have been transformative in the management of Human Immunodeficiency Virus (HIV) infection, altering the course of HIV/AIDS from a once-lethal condition to a chronic and manageable disease. Comprising a combination of different drug classes, ART inhibits viral replication at various stages of the HIV life cycle. Nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), integrase strand transfer inhibitors (INSTIs), and entry inhibitors collectively form the arsenal against HIV. The introduction of highly active antiretroviral therapy (HAART) marked a turning point, suppressing viral replication, preserving immune function, and significantly prolonging the lives of those living with HIV. Adherence to strict medication regimens is crucial to achieve viral suppression, prevent drug resistance, and reduce the risk of HIV transmission. As research continues, newer and more tolerable antiretroviral drugs emerge, promising enhanced efficacy and reduced side effects in the ongoing fight against HIV/AIDS.