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3 Integrase Inhibitors.....
  Raltegravir has been approved and on the market for a number of years and in now development in the phase 3 stage are 2 additional integrase inhibitors Gilead's elvitegravir and ViiV's dolutegravir both of which will be coformulated in a once daily one-pill per day. Dolutegravir will be coformulated with abacavir. Elvitegravir will be coformulated with tenofovir and boosted with the new Gilead booster cobicistat while dolutegravir is not boosted, and of course raltegravir is also unboosted. Below are the most recent studies reported for these 3 integrase inhibitors and as mentioned above raltegravir has been in the pharmacy for a number of years so the studies below include 4-5 years of raltegravir safety and antiviral activity. Dolutegravir has shown good activity in a number of patients with raltegravir resistance with more advanced data expected soon. Raltegravir is taken twice daily and is not coformulated. How will integrase inhibitors fit into the context of therapy decision making strategies for firstline initial therapy for treatment-naives and for subsequent treatment for 2nd and 3rd line therapy?

IAS: ViiV 'Next Generation' Integrase Dolutegravir, 48 Weeks SPRING-1 Study Naives - (07/21/11)

IAS: Safety Profile of Dolutegravir (DTG, S/GSK1349572), a Next Generation Integrase Inhibitor (INI) in Combination Therapy in Antiretroviral (ART)-naïve and ART-experienced Adults from Phase 2b Studies - (07/23/11)

Gilead Announces Two-Year Data From Pivotal Phase 3 Study of Elvitegravir, an Integrase Inhibitor for HIV - (12/12/11)

Gilead's Investigational Antiretroviral Quad (integrase Elvitegravir) Regimen Meets 48-Week Primary Objective in Pivotal Phase 3 Clinical Study 102 - (08/15/11)

IAS: Elvitegravir Once Daily is Non-Inferior to Raltegravir Twice Daily in Treatment-Experienced Patients: 48 Week Results From a Phase 3 Multicenter, Randomized Double-Blind Study - (07/20/11)

Efficacy and safety of once daily elvitegravir versus twice daily raltegravir in treatment-experienced patients with HIV-1 receiving a ritonavir-boosted protease inhibitor: randomised, double-blind, phase 3, non-inferiority study - published The Lancet - (10/24/11)

Randomized, phase 2 evaluation of two single-tablet regimens elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for the initial treatment of HIV infection - (04/23/11)

Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a dose-ranging, randomised, phase 2b trial - (10/24/11)

ICAAC: Dolutegravir vs Resistant Mutants: Selective Advantage Profiles of HIV-1 Integrase Mutants in the Presence of Dolutegravir - (09/26/11)

EACS: Dolutegravir (GSK/ViiV Integrase) Treatment (with 50mg Once & Twice Daily) of HIV Subjects with Raltegravir Resistance & 3-Class ART Resistance: viral suppression at Week 24 in the VIKING Study (10/17/11)

IAS: Sustained Efficacy and Tolerability of Raltegravir after 240 Weeks of Combination ART in Treatment-Naive HIV-1 Infected Patients: Final Analysis of Protocol 004 - (07/25/11)

EACS: Long-term Efficacy of Raltegravir or Efavirenz Combined with TDF/FTC in Treatment-naïve HIV-1-infected Patients: Week-192 Subgroup Analyses from STARTMRK (10/14/11)

ICAAC: Safety, Tolerability, and Efficacy of Raltegravir (RAL) in a Diverse Cohort of HIV-Infected Patients: 48-Week Results from the REALMRK Study - (09/22/11)

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