title: Recent Advances in Antiretroviral Agents: Potent Integrase Inhibitors.
abstract: Integrase strand transfer inhibitors (INSTIs) belong to a novel class of antiretroviral agents that have emerged as the new first-line treatments. Three such compounds are currently available, raltegravir, elvitegravir, dolutegravir and two more under development, bictegravir and cabotegravir. These compounds share the same mode of action but exhibit different pharmacokinetic/ pharmacodynamic properties, and drug-drug interactions. A series of studies in the past decade have established their efficacy compared to previous regimens, both in treatment- naïve and experienced patients. INSTIs have demonstrated a favorable safety profile with fewer adverse events and low rates of virological failure. Emergence of resistance to these agents, however, is a worrying concern, particularly for elvitegravir and raltegravir that display a lower genetic barrier than dolutegravir. On-going trials aim at establishing INSTIs as part of dual-drug HIV treatments or even monotherapy. New long-acting, injectable formulations are under investigation for treatment or prevention.
authors.affiliation: 1st Internal Medicine Department, Laiko General Hospital, National and Kapodistrian University of Athens, Agiou Thoma 17, Goudi, Athens, Greece.
authors.forename: Mina
authors.initials: M
authors.lastname: Psichogiou
authors.affiliation: Fourth Department of Medicine, Attikon General Hospital, National and Kapodistrian University of Athens, Athens, Greece.
authors.forename: Garyphalia
authors.initials: G
authors.lastname: Poulakou
authors.affiliation: First Department of Medicine, Laiko General Hospital, National and Kapodistrian University of Athens, Athens, Greece.
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Basoulis
authors.affiliation: Department of Hygiene Epidemiology and Medical Statistics, Medical School, National and Kapodistrian University of Athens, Athens, Greece.
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Paraskevis
authors.affiliation: Department of Pharmacy, Laiko General Hospital, Athens, Greece.
authors.forename: Antonios
authors.initials: A
authors.lastname: Markogiannakis
authors.affiliation: First Department of Medicine, Laiko General Hospital, National and Kapodistrian University of Athens, Athens, Greece.
authors.forename: George L
authors.initials: GL
authors.lastname: Daikos
mesh_terms: D044966:Anti-Retroviral Agents / Q000494:pharmacology / Q000627:therapeutic use*; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D015658:HIV Infections / Q000175:diagnosis / Q000188:drug therapy*; D019428:HIV Integrase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D000068898:Raltegravir Potassium / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D044966:Anti-Retroviral Agents; D003692:Delayed-Action Preparations; D019428:HIV Integrase Inhibitors; D000068898:Raltegravir Potassium
keywords: HIV; Integrase strand transfer inhibitors; adherence; efficacy; pharmacokinetics; resistance; tolerability