HIV-1 Integrase Inhibitor Resistance and Its Clinical Implications JOURNAL OF INFECTIOUS DISEASES Blanco, J., Varghese, V., Rhee, S., Gatell, J. M., Shafer, R. W. 2011; 203 (9): 1204-1214


With the approval in 2007 of the first integrase inhibitor (INI), raltegravir, clinicians became better able to suppress virus replication in patients infected with human immunodeficiency virus type 1 (HIV-1) who were harboring many of the most highly drug-resistant viruses. Raltegravir also provided clinicians with additional options for first-line therapy and for the simplification of regimens in patients with stable virological suppression. Two additional INIs in advanced clinical development-elvitegravir and S/GSK1349572-may prove equally versatile. However, the INIs have a relatively low genetic barrier to resistance in that 1 or 2 mutations are capable of causing marked reductions in susceptibility to raltegravir and elvitegravir, the most well-studied INIs. This perspective reviews the genetic mechanisms of INI resistance and their implications for initial INI therapy, the treatment of antiretroviral-experienced patients, and regimen simplification.

View details for DOI 10.1093/infdis/jir025

View details for Web of Science ID 000289306100002

View details for PubMedID 21459813

View details for PubMedCentralID PMC3069732