title: Role of raltegravir in HIV-1 management.
abstract: OBJECTIVE
  To review the literature concerning the role of raltegravir in the treatment of HIV-1 in antiretroviral (ARV)-experienced and ARV-naïve patients.
  
  
  METHODS
  A PubMed search was conducted for published data through March 2012 using the search terms raltegravir, MK-0518, and integrase strand transfer inhibitor. An additional search of International Pharmaceutical Abstracts for unpublished data, including data from the Infectious Diseases Society of America, the Conference on Retroviruses and Opportunistic Infections, the International AIDS Society, and the Interscience Conference on Antimicrobial Agents and Chemotherapy, was conducted using similar search terms.
  
  
  METHODS
  In vitro and in vivo Phase 2, Phase 3, and postmarketing studies available in English, evaluating antiretroviral regimens that contain raltegravir for the treatment of HIV-1 infection in both ARV-naïve and ARV-experienced patients, were evaluated. Studies assessing raltegravir pharmacokinetics and pharmacodynamics were included for review.
  
  
  RESULTS
  The nucleoside-based regimen of raltegravir with tenofovir/emtricitabine provides an effective first-line treatment option. However, nucleoside-sparing regimens appear unfavorable in ARV-naïve subjects and should be reserved for patients with limited treatment options. Raltegravir used with optimized background therapy provides an alternative regimen for ARV-experienced patients. This review describes the available in vitro and in vivo data on raltegravir potency, defined as the ability to achieve undetectable viral load, and safety profile, as well as comparison to standard HIV-1 therapies.
  
  
  CONCLUSIONS
  Raltegravir has demonstrated potent antiretroviral activity against HIV-1 in both ARV-naïve and ARV-experienced subjects, with the benefits of a favorable adverse effect profile and minimal drug interactions. Raltegravir must be dosed twice daily, as once daily raltegravir displays decreased virologic efficacy compared to twice daily dosing. However, the ongoing development of new integrase strand transfer inhibitors may provide potent once daily regimens.
authors.affiliation: South Carolina College of Pharmacy, University of South Carolina Campus, Columbia, USA.
authors.forename: Kristina E E
authors.initials: KE
authors.lastname: Rokas
authors.forename: P Brandon
authors.initials: PB
authors.lastname: Bookstaver
authors.forename: Caitlin L
authors.initials: CL
authors.lastname: Shamroe
authors.forename: S Scott
authors.initials: SS
authors.lastname: Sutton
authors.forename: Vanessa E
authors.initials: VE
authors.lastname: Millisor
authors.forename: Jacquelyn E
authors.initials: JE
authors.lastname: Bryant
authors.forename: Sharon B
authors.initials: SB
authors.lastname: Weissman
mesh_terms: D000225:Adenine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000627:therapeutic use; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000627:therapeutic use; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000627:therapeutic use; D004359:Drug Therapy, Combination; D000068679:Emtricitabine; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D019428:HIV Integrase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015497:HIV-1 / Q000302:isolation & purification; D006801:Humans; D063065:Organophosphonates / Q000008:administration & dosage / Q000627:therapeutic use; D011760:Pyrrolidinones / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000068898:Raltegravir Potassium; D000068698:Tenofovir
chemical_list: D019380:Anti-HIV Agents; D019428:HIV Integrase Inhibitors; D063065:Organophosphonates; D011760:Pyrrolidinones; D003841:Deoxycytidine; D000068898:Raltegravir Potassium; D000068698:Tenofovir; D000068679:Emtricitabine; D000225:Adenine