Ritonavir-boosted protease inhibitors in HIV therapy

Abstract

The advent of combination antiretroviral therapy has led to significant improvement in the care of HIV-infected patients. Originally designed as a protease inhibitor (PI), ritonavir is currently exclusively used as a pharmacokinetic enhancer of other protease inhibitors, predominantly due to ritonavir's potent inhibition of the cytochrome P450 3A4 isoenzyme. Ritonavir-boosting of PIs decrease pill burden and frequency of dosing. Boosted PIs are recommended for first-line therapy in treatment and play a key role in the management of treatment-experienced patients. Potential problems associated with PIs include metabolic abnormalities (e.g. dyslipidemia), increased cardiovascular risk, and drug interactions.

Key words::

• Antiretroviral therapy
• HIV
• protease inhibitors
• ritonavir

Declaration of interest: Dr Julio Montaner has received grants from, served as an ad hoc advisor to Abbott, Argos Therapeutics, Bioject Inc., Boehringer Ingelheim, BMS, Gilead Sciences, GlaxoSmithKline, Hoffmann-La Roche, Janssen-Ortho, Merck Frosst, Panacos, Pfizer, Schering, Serono Inc., TheraTechnologies, Tibotec (J&J), and Trimeris. Dr Montaner's program and research activities are supported by the Ministry of Health Services and the Ministry of Healthy Living and Sport, from the Province of British Columbia; through a Knowledge Translation Award from the Canadian Institutes of Health Research (CIHR); and through an Avant-Garde Award (No. 1DP1DA026182-01) from the National Institute of Drug Abuse, at the US National Institutes of Health.

Dr Mark Hull has received honoraria for speaking engagements and/or consultancy meetings from Merck Frosst, Pfizer, Janssen-Ortho, Gilead Sciences, and Sepracor Pharmaceuticals Inc. He has been a co-investigator on grants supported in part by Wyeth Pharmaceuticals.