Integrase is a viral enzyme that inserts the HIV virus into a healthy cell. Integrase inhibitors block the action of insertion and help to stop the duplication.
DHHS Status:Recommended in Combination as Initial Regimen for Most People with HIV
FDA approval date: October 12, 2007
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The standard dose of Isentress is one 400mg tablet taken twice a day. It can be taken with or without food. A pediatric formulation is approved in a 25mg and 100mg chewable tablet. The standard dose of Isentress HD is two 600mg tablets taken once daily for those new to therapy or having an undetectable viral load on an initial regimen of Isentress.
Review: Isentress was the first approved integrase inhibitor and is listed as “Recommended in Combination as initial regimen for most people with HIV” in the DHHS guidelines. Isentress was first introduced as “salvage” therapy for treatment-experienced patients. In combination with Truvada, it has been shown to be an option for those who have developed resistance to Non-Nucleoside Reverse Transcriptase Inhibitor regimens. It is a very good drug with low toxicity and virtually no side effects. The only slight drawback for some is the twice-a-day dosing, however the two 600mg tablets that can be taken once daily was approved in 2017, Isentress HD, and it is also “ Recommended in Combination as initial regimen for most people with HIV” according to the recent DHHS guidelines. Isentress is also recommended during pregnancy.
There are currently two much newer integrase inhibitors approved by the FDA as well in 2014 that are also both considered “ Recommended in Combination as initial regimen for most people with HIV” in the current DHHS guidelines, Tivicay (Dolutegravir), which is also included in the single tablet regimen Triumeq and another Vitekta (Elvitegravir) that is included in single tablet regimens, Stribild and Genvoya.
DHHS Status: Recommended in Combination as Initial Regimen for Most People with HIV
FDA approval date: August 12, 2013
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Tivicay is available in a 50mg tablet taken once daily for those on therapy for the first time or those with no previous Integrase Inhibitor use. One tablet, twice a day for those with Integrase Inhibitor drug resistance or those also taking Sustiva, Lexiva and Norvir, Aptivus and Norvir or Rifampin. Tivicay is approved for those 12-years and older weighing over approximately 88-pounds and can be taken without regard to meals.
Review: Tivicay was approved by the FDA in August of 2013 and is listed as “ Recommended in Combination as initial regimen for most people with HIV” in the current DHHS guidelines. Tivicay is shown in studies to be effective with few side effects and doesn’t require a booster. Tivicay is a second-generation Integrase Inhibitor which means Tivicay also can be effective for many who have developed a resistance to other drugs in the Integrase Inhibitor class such as Isentress, although dosing is doubled for these individuals.
Tivicay is available in combination with Epivir (Lamivudine) and Ziagen (Abacavir) for the single tablet regimen, Triumeq which received FDA approval on August 22nd of 2014 and is “Recommended Initial Regimen for Most People with HIV” in current DHHS guidelines for first time therapy. It is also in combination with Edurant to form the newer STR, Juluca. Pediatric DHHS guidelines added Tivicay in 2017 as part of a preferred regimen.
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