Drug treatment of human immunodeficiency virus (HIV) infection is a rapidly changing field. Practice changes as new drugs become available, results of studies are published, and clinical experience is accumulated. Accordingly, any review is likely to be outdated from the moment it is submitted, even before publication. In addition, the limitations inherent to a single review article of this length preclude in depth treatment of many important topics, including antiviral resistance testing and therapeutic drug monitoring. Other areas are not even addressed, such as treatment of special populations (including infants, children and pregnant women), “alternative therapy”, and use of HIV chemotherapeutics for perinatal, parenteral, or sexual postexposure prophylaxis. Nonetheless, every effort has been made to provide both a historical perspective and the most up-to-date information available on currently approved antiretroviral drugs, promising drug candidates in development, the status of laboratory monitoring pertinent to treatment and current treatment strategies for the HIV-infected adult patient. This review should serve as a useful summary for those now entering the field or seeking an overview of the current status of the chemotherapy of HIV infection.