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Protease Inhibitors

Protease is a protein-cleaving or cutting enzyme. The enzyme cuts proteins and allows them to reassemble for new copies of the HIV virus. PIs prevent the replication by inhibiting the protease enzyme's activity.


REYATAZ

(Atazanavir)

Manufacturer: Bristol-Myers Squibb (www.bms.com) Reyataz (www.reyataz.com)

FDA approval date: June 20, 2003

Financial Assistance: https://www.bms3assist.com/bms3assist/

A standard dose of Reyataz is one 300mg capsule and one 100mg Norvir capsule or 150mg of Tybost, taken with food once a day. Those who cannot tolerate Norvir can take two 200mg capsules of Reyataz with food once a day, as an alternative.

Review: Reyataz was downgraded to an “Alternative” regimen by the DHHS in their current guidelines mostly due to some side effect problems with mild jaundice and tolerability issues. Reyataz is usually boosted with Norvir (ritonavir). If the boosting agent, Norvir, is hard to tolerate by some, Reyataz can be used by itself in higher doses. The good news for Reyataz is that it received FDA approval on January 29th of last year in combination with a newer, approved PK Enhancer, Tybost (cobicistat) which is a built-in booster. The newly formulated and approved drug is Evotaz (see next). This formulation lessens the pill burden and also eliminates the need for Norvir.

The pluses for Reyataz are that it has a very convenient dosing, there is less diarrhea associated with it and Reyataz doesn’t seem to raise your cholesterol and triglyceride levels the way most other protease inhibitors do. In fact, one study suggests that Reyataz may actually increase your HDL (good) cholesterol, which helps protect you from heart disease.

Reyataz can be taken by women who are pregnant and is “Recommended” for use during pregnancy according to the DHHS guidelines. Reyataz can also be taken in combination with Norvir by children aged 6 and older.


EVOTAZ

(Atazanavir/Cobicistat)

Manufacturer: Bristol-Myers Squibb (www.bms.com) Evotaz (www.evotaz.com)

FDA approval date: January 29, 2015

Financial Assistance: https://www.evotaz.bmscustomerconnect.com/patients-caregivers/assistance-program

A standard dose of EvoTaz is one tablet (300mg atazanavir/150mg cobicistat) once daily with food.

Review:EvoTaz was approved by the FDA January 29th of last year and is listed as an Alternative HIV therapy in the current DHHS guidelines. Atazanavir, it’s key component, had been recommended for years and just downgraded to alternative status last year and Tybost (cobicistat) as been approved since 2014.

EvoTaz uses the recently approved PK Enhancer, Tybost (cobicistat) as a built-in booster. This eliminates the need for the stand alone booster Norvir. The built-in booster Tybost is a more tolerable formulation for those who have trouble with Norvir plus it lowers pill burden and lessens co-pays.


PREZISTA

(Darunavir)

Manufacturer: Janssen Therapeutics (www.janssentherapeutics.com)
Prezista (www.prezista.com)

FDA approval date: June 23, 2006

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

The standard dose of Prezista for people just starting treatment and the treatment-experienced without Prezista-related resistance is one 800mg tablet plus one 100mg Norvir capsule once-a-day. For treatment experienced patients who have had Prezista-related resistance or women who are pregnant, it is one 600mg tablet and one 100mg Norvir capsule twice a day. Prezista should be taken with food and should always be taken with Norvir. 75mg and 150mg tablets are available for children 3-years old and older, dosage is based in the child’s weight.

Review: Prezista boosted with Norvir is listed as a “Recommended” drug in the latest DHHS guidelines. Prezista, in combination with Norvir and Truvada is the only PI recommended for initial therapy in the DHHS treatment guidelines. Unlike, Reyataz, Prezista should not be taken without Norvir as a booster. Prezista, on January 29th of last year, was approved in combination with Gilead Science’s pharmacokinetic enhancer drug, Tybost (cobicistat) as Prezcobix (see next). This formulation will reduce the pill burden, some co-pay expenses and also help people who don’t tolerate Norvir well.

Prezista is available in an oral solution which can be preferable for children and people who have problems swallowing pills but it must also be boosted with Norvir.


PREZCOBIX

(Darunavir/Cobicistat)

Manufacturer: Janssen Therapeutics (www.janssentherapeutics.com)
Prezcobix (www.prezcobix.com)

FDA approval date: January 29, 2015

Financial Assistance: https://www.prezcobix.com/hcp/patient-savings-program

A standard dose of Prezcobix is one tablet (800mg darunavir/150mg cobicistat), once daily with food, in patients with no darunavir drug resistance.

Review: Prezcobix was approved by the FDA on January 29th of last year and is rated by the DHHS in their current guidelines as an Alternative HIV therapy. The key component of Prezcobix, Prezista (darunavir) is DHHS “Recommended” and Tybost (cobicistat) received approval as a pharmacokinetic (PK) enhancer last year.

Tybost has been formulated as a single pill with both Reyataz to form EvoTaz and with Prezista in this case to form Prezcobix. In both, it will help people who do not tolerate Norvir well (especially with Prezista since the addition of Norvir is a must), help with pill burden by reducing down to just one pill and will help with the co-pay and expense of eliminating Norvir.


KALETRA

(Lopinavir/Ritonavir)

Manufacturer: AbbVie (www.abbvie.com) Kaletra (www.kaletra.com)

FDA approval date: September 15, 2000

Financial Assistance: https://www.abbviepaf.org

Kaletra can be taken in tablets containing 200mg/50mg, two tablets, twice a day or four tablets once a day. Also three tablets can be taken twice a day by treatment experienced patients and women who are in their second and third trimester of pregnancy.

Review: Kaletra is no longer considered to be an “alternative” drug by the DHHS but rather an “Other” option. The DHHS states the “other” categorization as: Regimens that, in comparison with Recommended and Alternative regimens, may have reduced virologic activity, limited supporting data from large comparative clinical trials, or other factors such as greater toxicities, higher pill burden, drug interaction potential, or limitations for use in certain patient populations. Kaletra is the only PI with Norvir incorporated as a booster. While not as popular as Reyataz and Prezista it will most likely become even less used due to the Tybost co-formulations with both to form EvoTaz and Prezcobix respectively. Kaletra was an important drug at one time but just isn’t prescribed much anymore in the U.S. It has also been downgraded to an alternative during pregnancy.


NORVIR

(Ritonavir)

Manufacturer: AbbVie (www.abbvie.com) Norvir (www.norvir.com)

FDA approval date: March 1, 1996

Financial Assistance: https://www.abbviepaf.org

Norvir comes in 100mg tablet and gelatin capsules and 80mg/mL oral solution. Recommended dose is 600mg (6 capsules) every 12 hours which is almost never prescribed anymore. Lower doses of 100mg and 200mg when used as a boosting agent.

Review: Although Norvir is still approved as a PI, nobody really uses it for that anymore. Norvir is used as a “booster” for other PIs which helps keep the PI active in your blood longer. Gilead Science’s pharmacokinetic enhancer, Tybost (cobicistat) which was approved by the FDA in September of 2014, is a substitute boosting agent and has been approved in combination with Reyataz to form EvoTaz and Prezista to form Prezcobix both in single pill form. The introduction and approval of Tybost can potentially help many with the side effects of Norvir.


LEXIVA

(Fosamprenavir)

Manufacturer: ViiV Healthcare (www.viivhealthcare.com)
Lexiva (www.viivhealthcare.com)

FDA approval date: October 20, 2003

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

The standard dose of Lexiva is two 700mg pills twice a day; two 700mg tablets with two 100mg capsules of Norvir once daily; or one 700mg tablet with one 100mg capsule of Norvir twice daily. You can take it with or without food.

Review: The current DHHS guidelines classify Lexiva as “Not Recommended.”

Lexiva is a “prodrug” of Agenerase (amprenavir), a protease inhibitor that was approved by the FDA in 1999. Basically, Lexiva turns into Agenerase in your body. The big advantage is in the dosing. The standard dose of Agenerase was 16 huge pills a day. Lexiva’s dosing was far more convenient with fewer side effects. Current guidelines however, have dropped and do not recommend unboosted (not used with Norvir) Lexiva because of potential cross-resistance with the “recommended” PI, Prezista.


INVIRASE

(Saquinavir)

Manufacturer: Genentech (www.gene.com) Invirase (www.gene.com)

FDA approval date: December 6, 1995

Financial Assistance: N/A

The standard dose is 1,000mg (two 500mg capsules) twice daily, combined with 100mg of Norvir twice daily. It should be taken with food.

Review: Invirase is the hard gel version of Fortovase and basically replaced it. Invirase has been listed as “Not Recommended” in the current DHHS guidelines and is hardly prescribed anymore in the U.S. It’s patent expired in 2011.


VIRACEPT

(Nelfinavir)

Manufacturer: ViiV Healthcare (www.viivhealthcare.com)
Viracept (www.viivhealthcare.com)

FDA approval date: March 14, 1997

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

The standard dose of Viracept is five 250mg pills twice a day or two 625mg pills twice a day. Food increases the levels of Viracept in your blood, so take it with a meal.

Review: Viracept is listed by the DHHS guidelines as “Not Recommended.” It is an old drug, approved in 1997 and is infamous for causing diarrhea. It is not as strong or long-lasting as other PIs in the category.


CRIXIVAN

(Indinavir)

Manufacturer: Merck Healthcare (www.merck.com) Crixivan (www.merck.com)

FDA approval date: March 13, 1996

Financial Assistance: N/A

Crixivan comes in 200, 333 and 400mg capsules. Recommended dose is 800mg (two 400mg capsules) every eight hours or two 400mg capsules with either one or two 100mg Norvir capsules twice a day. It should be taken on an empty stomach or with a light meal.

Review: Crixivan is an old drug that was important in it’s time but it is rarely used anymore. It is no longer recommended for initial therapy by the DHHS.


APTIVUS

(Tipranavir)

Manufacturer: Boehringer-Ingelheim (www.boehringer-ingelheim.com)
Aptivus (www.boehringer-ingelheim.comm)

FDA approval date: June 25, 2005

Financial Assistance: https://www.us.boehringer-ingelheim.com/our_responsibility/patients-families/patient_assistance_program_information.html

The standard dose of Aptivus is 500mg (two 250mg capsules, twice a day), plus 200mg twice daily of Norvir. It should be taken with food.

Review: Aptivus is rarely used but when used, is salvage therapy for people who have tried and failed other HIV regimens. It is always used with Norvir. If Aptivus is prescribed, because of the risk of liver damage, your doctor should give you a liver function test before and periodically during treatment.



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!