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Integrase Inhibitor

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.


ISENTRESS

(Raltegravir)

Manufacturer: Merck (www.merck.com)
Isentress (www.isentress.com)

FDA approval date: October 12, 2007

Financial Assistance: https://www.merckhelps.com

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.

Review: Isentress was the first approved integrase inhibitor and is listed as “Recommended” 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.

There are currently two much newer integrase inhibitors approved by the FDA as well in 2014 that are also both considered “Recommended” in the current DHHS guidelines, Tivicay (Dolutegravir), which is also included in the single tablet regimen Triumeq and another Vitekta (Elvitegravir) that is included single tablet regimens, Stribild and Genvoya.


TIVICAY

(Dolutegravir)

Manufacturer: Viiv Healthcare (www.viivhealthcare.com)
Tivicay (www.tivicay.com)

FDA approval date: August 12, 2013

Financial Assistance: https://www.viivhealthcareforyou.com

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 the current DHHS guidelines. While relatively new, it 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 also “Recommended” in current DHHS guidelines for first time therapy. Tivicay is also presently being studied for pediatric use in children 6-weeks to 12-years.


VITEKTA

(Elvitegravir)

Manufacturer: Gilead Sciences (www.gilead.com)
Vitekta (www.vitekta.com)

FDA approval date: September 24, 2014

Financial Assistance: https://www.gileadcopay.com

A standard dose of Vitekta is one 85mg tablet once a day when taken with Reyataz 300mg/Norvir 100mg or Kaletra or one 150mg tablet once a day when taken with Prezista 600mg/Norvir 100mg twice daily, Lexiva 700mg/Norvir 100mg twice daily, or Aptivus 500mg/Norvir 200mg twice daily, in antiretroviral treatment-experienced adults. Take with food.

Review: Elvitegravir was approved by the FDA in September of 2014 and is the newest entry in the integrase inhibitor market which currently only has Isentress and Tivicay as the other approved drugs in this class of HIV drug. Elvitegravir is listed as “Recommended” in the current DHHS guidelines for first time use and is available in combination as the integrase inhibitor included in DHHS “Recommended” Single-tablet regimen, Stribild along with Cobicistat, Emtricitabine and Tenofovir and in another “Recommended” single-tablet regimen, Genvoya where it is combined with Cobicistat, Emtricitabine, and Tenofovir Alafenamide.

Elvitegravir can be used by treatment-experienced patients however, if there is a resistance to Isentress, patients are likely to have a resistance to Elvitegravir as well. Vitekta must also be used with a booster.



Single Tablet Regimens

Protease Inhibitors

Nucleoside Reverse Transcriptase Inhibitors

Non-Nucleoside Reverse Transcriptase Inhibitors

Fusion Inhibitor

Entry Inhibitor

Integrase Inhibitor

Pharmacokinetic Enhancer

 


 

 

 

 

 

 

 

 





Copyright 2017, Positive Health Publications, Inc.

This magazine is intended to enhance your relationship with your doctor - not replace it! Medical treatments and products should always be discussed with a licensed physician who has experience treating HIV and AIDS!