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Lexiva (fosamprenavir calcium)

Lexiva Tablet

Articles on Lexiva
Full US Prescribing Inormation
Patient Brochure

Patient Information
• Important Safety Information
• Drug Interactions
• Dosing
• Resistance Profile
• www.lexiva.com

Articles on Lexiva

Efficacy and Safety of Fosamprenavir + Ritonavir (FPV/RTV) 700mg/100mg Twice Daily (BID) Versus FPV/RTV 1400mg/100mg Once Daily (QD) with ABC/3TC QD over 24 Weeks - 11/05/2008

Limb and Trunk Fat Changes by Total Body DEXA After 96 Weeks of Treatment with Once Daily (QD) Fosamprenavir (FPV) Boosted with either 100 mg or 200 mg of Ritonavir (/r) plus Abacavir (ABC)/Lamivudine(3TC): COL100758 - 11/05/2008

Week 96 Virology Analysis of COL100758, a Study of Once-Daily (QD) Fosamprenavir (FPV) Boosted with 100 mg or 200 mg Ritonavir (/r) with Abacavir /Lamivudine (ABC/3TC) in Antiretroviral Naīve HIV-infected Patients - 11/05/2008

Long-Term Efficacy and Safety of Abacavir/Lamivudine (ABC/3TC) with Fosamprenavir + Ritonavir Versus Lopinavir/Ritonavir (LPV/r) over 144 Weeks - 11/05/2008

Switching from a 200mg-Ritonavir (RTV, r)-Boosted Fosamprenavir (FPV) Regimen (700mg/100mg BID or 1400mg/200mg QD) to a 100mg RTV-Boosted FPV Regimen (1400mg/100mg QD) Yields Similar Efficacy and Safety (the LESS Trial) - 11/05/2008

Once Daily Fosamprenavir (Lexiva) Boosted with Either 100 mg or 200 mg Ritonavir (Norvir): Efficacy Results from COL100758 - 11/03/07

FDA Approves Once-daily Fosamprenavir (Lexiva) Boosted with a Lower Once-daily Dose (100 mg) of Ritonavir - 10/16/07

Once-daily 1400/100 mg Dose of Fosamprenavir/ritonavir (Lexiva) Is Virologically Effective and Causes Fewer Body Fat Changes than 1400/200 mg Dose - 8/24/07

Once-daily Ritonavir-boosted Fosamprenavir (Lexiva) or Atazanavir (Reyataz), Both with Tenofovir/emtricitabine in Treatment-naive Patients: 48-week Results of the ALERT Trial - 8/03/07

FDA Approves Protease Inhibitor Fosamprenavir (Lexiva) for Treatment of HIV in Children - 6/22/07

Safety and Antiviral Activity of Fosamprenavir-containing Regimens in HIV-infected 2- to 18-Year-Old Pediatric Subjects - 3/16/07

Safety and Antiviral Activity of Fosamprenavir/Ritonavir (FPV/RTV) QD Regimens in HIV-Infected Pediatric Subjects Ages 2 to 18 Years (48 week Interim Data, Study APV20003) 3/16/07

Safety and Antiviral Activity of Fosamprenavir (FPV)-Containing Regimens in HIV-Infected 2 to 18 Year Old Pediatric Subjects (Interim Data, Study APV29005) 3/16/07

GlaxoSmithKline Offers Savings Program for Patients Purchasing Fosamprenavir 2/13/07

Once-daily boosted fosamprenavir (FPV/r) or atazanavir (ATV/r) with tenofovir (TDF)/emtricitabine (FTC) in antiretroviral naive HIV-1 infected patients: 24-week 11/27/06 .

Fosamprenavir/ritonavir (FPV/r): decrease of liver enzymes in patients co-infected with hepatitis C 11/27/06

Success of an induction-maintenance strategy using boosted fosamprenavir plus zidovudine and lamivudine for treating HIV-1 infected drug-naive subjects 11/27/06

Fosamprenavir boosted with a single 100 mg capsule of ritonavir as part of a once daily first line regimen in naive patients 11/27/06

Sustained virologic and immunologic response over 180 weeks in antiretroviral therapy (ART)-naīve subjects receiving fosamprenavir/ritonavir (FPV/r) QD 11/27/06

Lexiva - Important Safety Information

	You should not take LEXIVA if you have had an allergic reaction to LEXIVA or AGENERASE^Ž (amprenavir).
	High blood sugar, diabetes or worsening of diabetes, and bleeding in hemophiliacs have occurred in some patients taking protease inhibitors.
	When you start taking HIV medicines, your immune system may get stronger and could begin to fight infections that have been hidden in your body, such as pneumonia, herpes virus, or tuberculosis. If you have new symptoms after starting your HIV medicines, be sure to tell your doctor.
	Changes in body fat may occur in some patients taking antiretroviral therapy. The cause and long-term health effects of these conditions are not known at this time.
	Skin rashes can occur in patients taking LEXIVA. Rarely, rashes were severe or life threatening.
	Opportunistic infections can develop when you have HIV and your immune system is weak. It is very important that you see your healthcare provider regularly while you are taking LEXIVA to discuss any side effects or concerns.
	Most common side effects in clinical studies were diarrhea, headache, nausea, rash, and vomiting. In most cases, these side effects did not cause people to stop taking their medicine.

Lexiva - Drug Interactions

	LEXIVA should not be taken with: AGENERASE^Ž (amprenavir), Halcion^Ž (triazolam), ergot medications (Cafergot^Ž, Migranal^Ž, D.H.E. 45^Ž, and others), Propulsid^Ž (cisapride), Versed^Ž (midazolam), Orap^Ž (pimozide), Zocor^Ž (simvastatin), Mevacor^Ž, (lovastatin), Rifadin^Ž (rifampin), Rescriptor^Ž (delavirdine mesylate), or St. John's wort (Hypericum perforatum). If you are taking Norvir^Ž (ritonavir), you should not take Tambocor^Ž (flecainide), or Rythmol^Ž (propafenone hydrochloride).
	Serious and/or life-threatening events could occur between LEXIVA and other medications, including Cordarone^Ž (amiodarone), lidocaine (intravenous only), Elavil^Ž (amitriptyline HCl) and Tofranil^Ž (imipramine pamoate), tricyclic antidepressants, and Quinaglute^Ž (quinidine).
	Women who use birth control pills should choose a different kind of contraception. LEXIVA can affect the safety and effectiveness of birth control pills.
	Patients taking Viagra^Ž (sildenafil citrate) or LEVITRA^Ž (vardenafil HCl) with LEXIVA may be at an increased risk of side effects.
	This list of drug interactions is not complete. Be sure to tell your healthcare provider about all medicines you are taking or plan to take, including over-the-counter drugs, vitamins, and herbals.

Lexiva - Dosing

Your healthcare provider may prescribe LEXIVA for you either once a day or twice a day, based on your HIV treatment history. Often LEXIVA can be taken at the same time you take your other HIV medicines.

When LEXIVA is prescribed with ritonavir, this is known as "boosting" the dose of LEXIVA. Boosting with ritonavir increases the amount of LEXIVA in your body. And boosting may give your healthcare provider the option of prescribing LEXIVA once or twice a day. LEXIVA, with or without ritonavir, is only 4 pills a day.

Whatever regimen you are prescribed, remember: always take your HIV medicines exactly as your healthcare provider tells you to.

*Once daily with ritonavir is not recommended for PI-experienced patients.

Lexiva - Resistance Profile

ART-naive patients
LEXIVA/r, QD no primary or
secondary protease mutations

APV30002 (SOLO) a randomized, open-label study of LEXIVA/r (1400/200 mg) QD vs NFV (1250 mg) BID in combination with ABC/3TC BID in 649 ART-naive patients.

Because the potential for HIV cross-resistance among protease inhibitors has not been fully explored, it is unknown what effect therapy with LEXIVA will have on the activity of subsequently administered protease inhibitors.

Clinical relevance of resistance data is currently being evaluated.

* Excludes patients without paired genotypes at baseline and at the time that virologic failure was first detected.
Common natural polymorphisms in the absence of other PRO mutations are excluded: NFV n = 3 [M36 m/l, K20k/m, L10l], LEXIVA/r n = 1 [V77v/i].

ART-naive patients
LEXIVA, BID limited cross-resistance

APV30001 (NEAT) a randomized, open-label study of LEXIVA (1400 mg) BID vs NFV (1250 mg) BID in combination with ABC/3TC BID in 249 ART-naive patients.

Excludes patients without paired genotypes at baseline and at the time that virologic failure was first detected.

^§ Common natural polymorphisms in the absence of other PRO mutations are excluded: LEXIVA n = 1 [A71a/t].

LEXIVA/r provides a high genetic barrier to the development of resistance at 48 weeks

ē	No PRO mutations
ē	Very low incidence of RT mutations no K65R mutations

LEXIVA, BID limited cross-resistance¹

	APV30001 (NEAT) a randomized, open-label study of LEXIVA (1400 mg) BID vs NFV (1250 mg) BID in combination with ABC/3TC BID in 249 ART-naive patients.
Excludes patients without paired genotypes at baseline and at the time that virologic failure was first detected. ^§ Common natural polymorphisms in the absence of other PRO mutations are excluded: LEXIVA n = 1 [A71a/t].

	No significant difference in incidence of PRO or RT mutations for LEXIVA vs NFV
	At the time of first treatment failure, PRO mutations I54L/M or V32I + I47V were selected by LEXIVA. These mutations result in limited cross-resistance to other PIs

PI-experienced patients

LEXIVA/r, BID

	The following amprenavir resistance-associated mutations were selected either alone or in combination: V32I, M46I/L, I47V, I50V, I54L/M, and I84V
	Varying degrees of cross-resistance among HIV-1 protease inhibitors have been observed

APV30003 (CONTEXT) a randomized, open-label study of LEXIVA/r (1400/200 mg) QD or LEXIVA/r (700/100 mg) BID vs LPV/r (400 mg/100 mg) BID in combination with 2 NRTIs in 315 PI-experienced patients.

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Protease Inhibitors (PIs)

Note: Most PIs are now used
in combination with low-dose
ritonavir (Norvir)

Agenerase (amprenavir)

Aptivus (tipranavir)

Crixivan (indinavir)

Invirase (saquinavir )

Kaletra (lopinavir/ritonavir)

Lexiva (fosamprenavir)

Norvir (ritonavir)

Prezista (darunavir)

Reyataz (atazanavir)

Viracept (nelfinavir)

Nucleoside / Nucleotide
Reverse Transcriptase
Inhibitors (NRTIs)

Combivir (zidovudine + lamivudine)

Epivir (lamivudine; 3TC)

Emtriva (emtricitabine; FTC)

Epzicom (abacavir + lamivudine)

Retrovir (zidovudine; AZT)

Trizivir (abacavir + zidovudine +lamivudine)

Truvada (tenofovir + emtricitabine)

Videx (didanosine; ddI)

Viread (tenofovir)

Zerit (stavudine; d4T)

Ziagen (abacavir)

non Nucleoside
Reverse Transcriptase
Inhibitors (nNRTIs)

Intelence (etravirine)

Rescriptor (delavirdine)

Sustiva (efavirenz)

Viramune (nevirapine)

Entry / Fusion Inhibitors

Fuzeon (enfuvirtide)

Selzentry/Celsentri ( maraviroc)

Fixed-dose Combinations

Atripla (efavirenz + emtricitabine + tenofovir)

Combivir (zidovudine + lamivudine)

Trizivir (abacavir + zidovudine + lamivudine)

Truvada (tenofovir + emtricitabine)

Integrase Inhibitors

Isentress (raltegravir)