Because of the potential risk of toxicity from the large amount of the excipient, propylene glycol, contained in AGENERASE Oral Solution, that formulation is contraindicated in infants and children below the age of 4 years and certain other patient populations and should be used with caution in others. Consult the complete prescribing information for AGENERASE Oral Solution for full information.
PATIENT INFORMATION INCLUDED
AGENERASE (amprenavir) is an inhibitor of the human immunodeficiency virus (HIV) protease.
AGENERASE (amprenavir) is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.
The following points should be considered when initiating therapy with AGENERASE:
In a study of NRTI-experienced, protease inhibitor-naive patients, AGENERASE was found to be significantly less effective than indinavir.
Mild to moderate gastrointestinal adverse events led to discontinuation of AGENERASE primarily during the first 12 weeks of therapy (ADVERSE REACTIONS).
There are no data on response to therapy with AGENERASE in protease inhibitor-experienced patients.
Published Studies Related to Agenerase (Amprenavir)
Steady-state amprenavir and tenofovir pharmacokinetics after coadministration of unboosted or ritonavir-boosted fosamprenavir with tenofovir disoproxil fumarate in healthy volunteers. [2010.03]
Objective An open-label, three-period pharmacokinetic study was conducted to investigate the drug interaction potential between fosamprenavir (FPV) and tenofovir disoproxil fumarate (TDF). Methods Thirty-six healthy subjects received TDF 300 mg once daily (qd) for 7 days (period 1), and then were randomized to 14 days of either FPV 1400 mg twice daily (bid) or FPV/ritonavir (RTV) 700/100 mg bid alone or with TDF (period 2)...
Pharmacokinetics of concurrent administration of fosamprenavir and atazanavir without ritonavir in human immunodeficiency virus-negative subjects. [2009.08]
STUDY OBJECTIVE: To quantify the pharmacokinetics of amprenavir and atazanavir (administered as the prodrug fosamprenavir) alone and in combination in human immunodeficiency virus (HIV)-negative subjects... CONCLUSION: Atazanavir 400 mg/day plus fosamprenavir 1400 mg/day significantly decreased concentrations of atazanavir compared with standard dosing regimens of each drug alone. This dosing scheme is not a recommended combination of dual, fully active protease inhibitors.
Fosamprenavir/ritonavir in advanced HIV disease (TRIAD): a randomized study of high-dose, dual-boosted or standard dose fosamprenavir/ritonavir in HIV-1-infected patients with antiretroviral resistance. [2009.08]
BACKGROUND: APV102002 was an open-label study comparing a dual-boosted HIV-1 protease inhibitor (PI) [fosamprenavir/lopinavir/ritonavir (FPV/LPV/RTV; 1400 mg/533 mg/133 mg twice daily)] and a high dose of FPV/RTV 1400 mg/100 mg twice daily (HD-FPV/RTV) versus the standard FPV/RTV 700 mg/100 mg twice-daily (STD-FPV/RTV) regimen for 24 weeks... CONCLUSIONS: While the strategies of higher dose FPV/RTV and dual FPV/LPV/RTV were relevant at the time of study initiation, new therapies for antiretroviral-experienced patients make such strategies of limited interest. In addition, this study failed to demonstrate antiviral superiority of the HD-FPV/RTV or FPV/LPV/RTV regimen over the STD-FPV/RTV twice-daily regimen in highly treatment-experienced patients.
Fosamprenavir/ritonavir plus tenofovir does not affect amprenavir pharmacokinetics: no effect of tenofovir. [2007.06.19]
The effect of tenofovir disoproxil fumarate (TDF) in combination with two boosted fosamprenavir regimens on amprenavir pharmacokinetic parameters was assessed in this prospective phase I crossover study with 30 healthy volunteers.
Dose separation does not overcome the pharmacokinetic interaction between fosamprenavir and lopinavir/ritonavir. [2006.08]
Previous investigations have shown a significant negative two-way drug interaction between fosamprenavir (FPV) and lopinavir/ritonavir (LPV/RTV) in both human immunodeficiency virus (HIV)-infected patients and seronegative volunteers. This randomized, nonblinded, three-way crossover study of HIV-seronegative adult volunteers investigated dose separation and increased doses of RTV as a means to overcome the interaction between FPV and LPV/RTV...
Clinical Trials Related to Agenerase (Amprenavir)
A Study of Three Anti-HIV Drug Combinations in Patients Who Have Taken Amprenavir [Completed]
To determine the proportion of patients treated with amprenavir, zidovudine (ZDV), stavudine
(D4T) and lamivudine (3TC) whose HIV-1 RNA level remains below the level of detection during
96 weeks of therapy. To determine the proportion of patients treated with indinavir (IDV),
nevirapine (NVP), 3TC, and d4T whose HIV-1 RNA level decreases and then remains below the
level of detection, during the 96-week therapy period. To determine the viral effects,
safety, tolerability, and pharmacokinetics of amprenavir in combination with zidovudine,
stavudine, and lamivudine. [AS PER AMENDMENT 2/27/98: To determine the proportion of patients
with undetectable plasma HIV RNA, by treatment and baseline RNA cohort (either detectable or
undetectable). To determine the durability of these regimens by estimating the distribution
of time to loss of virologic suppression (or equivalently, time to virologic failure), by
treatment and baseline RNA cohort.] This study allows patients who have successfully
participated in ACTG 347 or other trials involving amprenavir to continue treatment with
amprenavir, ZDV, d4T, and 3TC. Additionally, this study provides patients whose HIV-1 RNA was
not reduced to undetectable levels or who had a significant increase in plasma levels
("treatment failures") the opportunity to change to a potentially more active regimen that
includes indinavir, nevirapine, lamivudine, and stavudine.
A Study of 141W94 Used Alone or in Combination With Zidovudine Plus 3TC in HIV-Infected Patients [Completed]
To determine the proportion of patients whose plasma HIV-1 RNA level remains below a
detectable level (less than 500/ml) after 24 weeks of study therapy with either 141W94
monotherapy or 141W94 plus zidovudine (ZDV) and lamivudine (3TC). To determine the safety and
tolerability of 141W94 monotherapy and the combination of 141W94 plus 3TC in patients with
Although dramatic inhibition of HIV-1 replication is achieved with ritonavir or indinavir
monotherapy, in both cases maximum suppression required combination treatment together with
nucleoside analog RT inhibitors. This study tests the hypothesis that monotherapy with
141W94 doses that result in Cmin levels far in excess of the IC90 corrected for plasma
protein binding for HIV-1 can achieve the same virologic and immunologic effects in terms of
magnitude and durability, as has been observed with combinations of other protease inhibitors
plus nucleoside analogs.
An Open-Label Study to Evaluate the Efficacy and Safety of Amprenavir (141W94) and Abacavir Combination Therapy in Protease Inhibitor Experienced Subjects With HIV-1 Infection Who Are Failing Their Current Antiretroviral Treatment Regimen [Completed]
To assess the safety, tolerance, and efficacy of amprenavir (APV) plus abacavir (ABC) in
patients who have previously failed antiretroviral treatment containing a protease inhibitor
(PI). To provide open-label, pre-approval access to APV for adults and adolescents with
HIV-1 infection and limited treatment options.
This study is being conducted to provide open-label APV to patients in danger of HIV disease
progression, as well as those who may benefit beyond the expected outcomes of current
anti-retroviral therapies. Despite unapproved status, APV may prove highly efficacious in
combatting HIV progression and may help those in need, prior to regulatory approval.
Four-Drug Combination Therapy With Zidovudine, Lamivudine, 1592U89 (Abacavir), and 141W94 (Amprenavir) in HIV-Infected Patients [Active, not recruiting]
The purpose of this study is to see if the multidrug combination of zidovudine (ZDV),
lamivudine (3TC), 1592U89 (abacavir [ABC]), and 141W94 (amprenavir [APV]) is a safe and
effective treatment for HIV-infected patients and if there is a reduction of active HIV in
blood and other tissues.
HIV infection is a life-changing illness and new HIV treatments must be tested. This study
will test if a 4-drug combination will reduce HIV virus activity in blood and other tissues
and if it is safe and well tolerated. Doctors also want to know if the multidrug combination
is able to decrease viral activity over a long time period.
A Study on Amprenavir in Combination With Other Anti-HIV Drugs in HIV-Positive Patients [Completed]
The purpose of this study is to compare 4 different combinations of anti-HIV drugs and to
determine the number of people whose HIV blood levels decrease to 200 copies/ml or less while
on the treatment. This study evaluates the safety of these drug combinations, which include
an experimental protease inhibitor (PI), amprenavir.
Despite the success that many patients have had with PI treatment regimens, there is still a
possibility that patients receiving PIs may continue to have high HIV blood levels. Because
of this possibility, alternative drug combinations containing PIs are being studied. It
appears that amprenavir, when taken with 3 or 4 other anti-HIV drugs, may be effective in
patients with prior PI treatment experience.
Page last updated: 2010-10-05