, Volume 70, Issue 14, pp 1885-1915
Date: 19 Sep 2012


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Lopinavir/ritonavir (Kaletra®) is an orally administered coformulated ritonavir-boosted protease inhibitor (PI) comprising lopinavir and low-dose ritonavir. It is indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection in adults, adolescents and children. Lopinavir/ritonavir is available as a tablet, soft-gel capsule and an oral solution for patients with difficulty swallowing.

In well designed, randomized clinical trials, lopinavir/ritonavir, in combination with other antiretroviral therapies (ART), provided durable virological suppression and improved immunological outcomes in both ART-naive and -experienced adult patients with virological failure. Furthermore, lopinavir/ritonavir demonstrated a high barrier to the development of resistance in ART-naive patients. More limited data indicate that it is effective in reducing plasma HIV-1 RNA levels in paediatric patients. Lopinavir/ritonavir has served as a well established benchmark comparator for the noninferiority of other ritonavir-boosted PI regimens. Although generally well tolerated, lopinavir/ritonavir is associated with generally manageable adverse gastrointestinal side effects and hypertriglyceridaemia and hypercholesterolaemia, which may require coadministration of lipid-lowering agents to reduce the risk of coronary heart disease.

Lopinavir/ritonavir, in combination with other ART agents, is a well established and cost-effective treatment for both ART-naive and -experienced patients with HIV-1 infection and, with successful management of adverse events, continues to have a role as an effective component of ART regimens for the control of HIV-1 infection.

Various sections of the manuscript reviewed by: B. Gazzard, Chelsea and Westminster Hospital, London, UK; F. Gutiérrez, Infectious Diseases and HIV Unit, Hospital General Universitario de Elche, Elche, Spain; J.D. Scott, Pharmacy Practice and Administration, Western University of Health Sciences, Pomona, California, USA; K.N. Simpson, Center for Health Economics and Policy Studies, Medical University of South Carolina, Charleston, South Carolina, USA.

Data Selection

Sources: Medical literature published in any language since 1980 on ‘lopinavir/ritonavir’, identified using MEDLINE and EMBASE, supplemented by AdisBase (a proprietary database). Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug.
Search strategy: MEDLINE and EMBASE search terms were ‘lopinavir ritonavir’ in title. AdisBase search terms were ‘lopinavir/ritonavir’ or ‘lopinavir-ritonavir’ or ‘ABT-378/ritonavir’. Searches were last updated on 2 September 2010.
Selection: Studies in patients with HIV-1 infection who received lopinavir/ritonavir. Inclusion of studies was based mainly on the methods section of the trials. When available, large, well controlled trials with appropriate statistical methodology were preferred. Relevant pharmacodynamic and pharmacokinetic data are also included.
Index terms: Lopinavir/ritonavir, HIV-1 infection, antiretroviral, boosted protease inhibitor, pharmacodynamics, pharmacokinetics, therapeutic use, tolerability.