Antiretroviral therapies have revolutionized the approach to HIV infection, providing a multifaceted strategy to impede viral replication and progression to AIDS. NRTIs, acting as nucleotide analogs, interrupt the reverse transcription process crucial for viral DNA synthesis. NNRTIs, binding to the reverse transcriptase enzyme, hinder its activity, while PIs disrupt the maturation of viral proteins. INSTIs, a newer class, block the integration of viral DNA into the host genome. Entry inhibitors prevent viral entry into host cells, offering additional layers of defense. The introduction of combination therapies has significantly enhanced treatment outcomes, reducing viral load and boosting immune function. Challenges persist, including issues of drug resistance, long-term side effects, and the need for lifelong adherence. The quest for long-acting formulations and innovative strategies, such as broadly neutralizing antibodies and therapeutic vaccines, continues to advance the field, raising hopes for improved HIV management and eventually achieving a cure.