title: Efficacy and Tolerability of Integrase Inhibitors in Antiretroviral-Naive Patients.
abstract: Integrase strand transfer inhibitors are a new class of antiretroviral agents recently licensed for the treatment of both naive and experienced HIV-infected patients. They inhibit the catalytic activity of the HIV-encoded enzyme integrase and prevent the integration of the HIV genome into the host cell genome, so slowing the propagation of the infection. Integrase strand transfer inhibitors cause a rapid drop in viral load, exhibit very low drug interactions (except elvitegravir/cobicistat), and have low pill burden and convenient dosing frequency. Drugs in this class have been compared to others in antiretroviral-naive patients with efavirenz and with protease inhibitors. Final results of the STARTMRK trial highlighted the better virologic and immunologic performance of raltegravir over efavirenz/emtricitabine/tenofovir disoproxil co-formulation. Raltegravir was also superior to atazanavir/ritonavir and darunavir/ritonavir in the ACTG 5257 study for the combined virologic/tolerability endpoint. Elvitegravir/cobicistat/emtricitabine/tenofovir was non-inferior to efavirenz/emtricitabine/tenofovir and to atazanavir/ritonavir plus emtricitabine/tenofovir in terms of confirmed virologic response in the GS-US-236-0102 and GS-US-236-0103 studies, respectively. Finally, dolutegravir showed non-inferiority compared to raltegravir in the SPRING-2 study and was superior to efavirenz and darunavir/ritonavir in the SINGLE and FLAMINGO trials, respectively. The aim of this review is to analyze the data on efficacy and safety of integrase strand transfer inhibitors in antiretroviral-naive HIV patients and discuss the strengths and weaknesses of drugs within this class.
authors.affiliation: Department of Immigration Diseases and HIV/AIDS, Unit for Immunodeficiencies and Infectious Diseases in Women, A.O. Dei Colli - Hospital for Infectious Diseases D. Cotugno, Naples, Italy.
authors.forename: Maurizio
authors.initials: M
authors.lastname: D'Abbraccio
authors.affiliation: Department of Immigration Diseases and HIV/AIDS, Unit for Immunodeficiencies and Infectious Diseases in Women, A.O. Dei Colli - Hospital for Infectious Diseases D. Cotugno, Naples, Italy.
authors.forename: Annunziata
authors.initials: A
authors.lastname: Busto
authors.affiliation: Department of Immigration Diseases and HIV/AIDS, Unit for Immunodeficiencies and Infectious Diseases in Women, A.O. Dei Colli - Hospital for Infectious Diseases D. Cotugno, Naples, Italy.
authors.forename: Mario
authors.initials: M
authors.lastname: De Marco
authors.affiliation: Department of Immigration Diseases and HIV/AIDS, Unit for Immunodeficiencies and Infectious Diseases in Women, A.O. Dei Colli - Hospital for Infectious Diseases D. Cotugno, Naples, Italy.
authors.forename: Mario
authors.initials: M
authors.lastname: Figoni
authors.affiliation: Department of Immigration Diseases and HIV/AIDS, Unit for Immunodeficiencies and Infectious Diseases in Women, A.O. Dei Colli - Hospital for Infectious Diseases D. Cotugno, Naples, Italy.
authors.forename: Adelaide
authors.initials: A
authors.lastname: Maddaloni
authors.affiliation: Department of Immigration Diseases and HIV/AIDS, Unit for Immunodeficiencies and Infectious Diseases in Women, A.O. Dei Colli - Hospital for Infectious Diseases D. Cotugno, Naples, Italy.
authors.forename: Nicola
authors.initials: N
authors.lastname: Abrescia
mesh_terms: D019380:Anti-HIV Agents / Q000008:administration & dosage* / Q000494:pharmacology; D004334:Drug Administration Schedule; D004338:Drug Combinations; D015658:HIV Infections / Q000188:drug therapy* / Q000276:immunology / Q000503:physiopathology; D015497:HIV-1 / Q000187:drug effects*; D006575:Heterocyclic Compounds, 3-Ring / Q000008:administration & dosage* / Q000494:pharmacology; D006801:Humans; D019429:Integrase Inhibitors / Q000008:administration & dosage* / Q000494:pharmacology; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D000068898:Raltegravir Potassium / Q000008:administration & dosage* / Q000494:pharmacology; D016032:Randomized Controlled Trials as Topic; D016896:Treatment Outcome; D019562:Viral Load / Q000187:drug effects*; D000099226:Dolutegravir
chemical_list: D019380:Anti-HIV Agents; D004338:Drug Combinations; D006575:Heterocyclic Compounds, 3-Ring; D019429:Integrase Inhibitors; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D000068898:Raltegravir Potassium; D000099226:Dolutegravir