HIV protease inhibitors: Present and future

Antiretroviral therapy offers many options, largely based on the next-generation protease inhibitors (PIs). Early PI-based treatments involve high pill burdens and dosing schedules, and concerns of long-term toxicities are well established. In patients who have already achieved viral suppression, novel agents and strategies should be used to simplify the dosing treatment, reduce adverse events or preserve drug options. In experienced patients, drug escalation between PIs and different associations between classes allow virological suppression to be reached in the majority of patients. Therefore, there is a persistent clinical need for the discovery and development of new protease inhibitors. Several firms are trying to develop new types of PIs that will not be cross-resistant with existing drugs and will not require ritonavir boosting. This article aims to offer an overview on present drug options recommended for treatment in naive and experienced patients, new strategies currently undergoing clinical evaluation and new compounds in the pipeline. © 2011 Future Medicine Ltd.