title: Update on raltegravir and the development of new integrase strand transfer inhibitors.
abstract: Raltegravir (RAL) is the first antiretroviral in the integrase strand transfer inhibitors (INSTI) class. The use of RAL has expanded since its approval in October 2007 for multidrug-resistant human immunodeficiency virus type 1 infection in adults. RAL is now a guideline-preferred treatment option for antiretroviral-naïve patients, indicated for treatment in adolescents, and is being studied as an integral part of nucleoside sparing regimens. The development of resistance and the need for a once-daily dosing option has led to the development of new INSTIs, including elvitegravir and dolutegravir. Elvitegravir is being studied in a promising once-daily single-tablet regimen with tenofovir, emtricitabine, and the investigational pharmacoenhancer cobicistat. The development of cobicistat and the new once-daily INSTIs may revolutionize the treatment of human immunodeficiency virus type 1 infection. This article reviews the current literature on raltegravir and new developments in the INSTI class.
authors: South Carolina College of Pharmacy and the Division of Infectious Diseases, Department of Internal Medicine, University of South Carolina School of Medicine, Columbia, SC, USA.
authors: Caitlin Lee
authors: CL
authors: Shamroe
authors: Paul Brandon
authors: PB
authors: Bookstaver
authors: Kristina E E
authors: KE
authors: Rokas
authors: Sharon B
authors: SB
authors: Weissman
mesh_terms: D015658:HIV Infections / Q000188:drug therapy*; D019428:HIV Integrase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D006575:Heterocyclic Compounds, 3-Ring / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D011760:Pyrrolidinones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D015363:Quinolones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D000068898:Raltegravir Potassium; D000099226:Dolutegravir
chemical_list: D019428:HIV Integrase Inhibitors; D006575:Heterocyclic Compounds, 3-Ring; D010078:Oxazines; D010879:Piperazines; D011728:Pyridones; D011760:Pyrrolidinones; D015363:Quinolones; D000068898:Raltegravir Potassium; D000099226:Dolutegravir; C509700:elvitegravir