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Review of the safety, efficacy, and pharmacokinetics of elvitegravir with an emphasis on resource-limited settings

Authors Lee JSF, Calmy A, Andrieux-Meyer I, Ford N

Received 17 October 2011

Accepted for publication 28 November 2011

Published 12 January 2012 Volume 2012:4 Pages 5—15


Review by Single-blind

Peer reviewer comments 2

Janice Soo Fern Lee1, Alexandra Calmy1,2, Isabelle Andrieux-Meyer1, Nathan Ford1,3
1Médecins Sans Frontières, 2HIV/AIDS Unit, Infectious Disease Service, Geneva University Hospital, Geneva, Switzerland; 3Centre for Infectious Disease Epidemiology and Research, University of Cape Town, South Africa

Abstract: Integrase inhibitors represent an important new class of antiretroviral drugs. Elvitegravir, the second available integrase inhibitor to be submitted for regulatory approval appears to be a promising once-daily agent when combined with other antiretroviral drugs. Elvitegravir has demonstrated good efficacy and safety, with minimal side effects and no specific requirements in terms of laboratory monitoring. In addition, elvitegravir is available as a fixed-dose combination. However, the drug requires boosting and this leads to a number of drug–drug interactions and necessary dose adjustment when dosing with certain drugs, including dose reduction in the presence of atazanavir, lopinavir, rifabutin, and ketoconazole, and dose increase for ethinyl estradiol when co-administered with boosted elvitegravir. The main advantage of elvitegravir lies in its potential to be administered as a once-daily, single pill. Limitations include dose adjustment requirements, a relatively low genetic barrier to resistance, high price, and lack of data for use in children. Clinical trials addressing specific challenges encountered in resources-limited settings should be encouraged.

Keywords: elvitegravir, efficacy, safety, resistance, resource-limited settings

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