PREZISTA™ (darunavir) is an inhibitor of the human immunodeficiency virus (HIV) protease. PREZISTA™ (darunavir), in the form of darunavir ethanolate, has the following chemical name: [(1 S,2 R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-
(phenylmethyl)propyl]-carbamic acid (3 R,3a S,6a R)-hexahydrofuro[2,3- b ]furan-3-yl ester monoethanolate.
PREZISTA, co-administered with 100 mg ritonavir (PREZISTA/rtv), and with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV) infection in antiretroviral treatment-experienced adult patients, such as those with HIV-1 strains resistant to more than one protease inhibitor.
This indication is based on Week 24 analyses of plasma HIV RNA levels and CD4+ cell counts from 2 controlled trials of PREZISTA/rtv in combination with other antiretroviral drugs. Both studies were conducted in clinically advanced, treatment-experienced (NRTIs, NNRTIs, and PIs) adult patients with evidence of HIV-1 replication despite ongoing antiretroviral therapy.
The following points should be considered when initiating therapy with PREZISTA/rtv:
- Treatment history and, when available, genotypic or phenotypic testing, should guide the use of PREZISTA/rtv (see MICROBIOLOGY).
- The use of other active agents with PREZISTA/rtv is associated with a greater likelihood of treatment response (see MICROBIOLOGY and INDICATIONS AND USAGE, Description of Clinical Studies).
- The risks and benefits of PREZISTA/rtv have not been established in treatment-naïve adult patients or pediatric patients.
Published Studies Related to Prezista (Darunavir)
96 week results from the MONET trial: a randomized comparison of darunavir/ritonavir with versus without nucleoside analogues, for patients with HIV RNA <50 copies/mL at baseline. [2011.08]
BACKGROUND: In virologically suppressed patients, switching to darunavir/ritonavir monotherapy could avoid resistance and adverse events from continuing nucleoside analogues. METHODS: Two hundred and fifty-six patients with HIV RNA <50 copies/mL on current antiretrovirals were switched to darunavir/ritonavir 800/100 mg once daily, either as monotherapy (n = 127) or with two nucleoside analogues (n = 129)...
Effects of tipranavir, darunavir, and ritonavir on platelet function, coagulation, and fibrinolysis in healthy volunteers. [2011.06.01]
The use of HIV protease inhibitors (PIs) as part of antiretroviral therapy in the treatment of HIV-1 infection may be associated with an increased risk of bleeding... There was large inter-patient variability in antiplatelet effect for all PI treatments, ranging from no effect to complete inhibition of AA-induced platelet aggregation.
Pharmacokinetic interactions of maraviroc with darunavir-ritonavir, etravirine, and etravirine-darunavir-ritonavir in healthy volunteers: results of two drug interaction trials. [2011.05]
The effects of darunavir-ritonavir at 600 and 100 mg twice daily (b.i.d.) alone, 200 mg of etravirine b.i.d... when coadministered with darunavir-ritonavir with or without etravirine.
Week 48 analysis of once-daily vs. twice-daily darunavir/ritonavir in treatment-experienced HIV-1-infected patients. [2011.04.24]
OBJECTIVE: ODIN (Once-daily Darunavir In treatment-experieNced patients) was a phase III, 48-week, open-label study comparing once-daily vs. twice-daily darunavir/ritonavir (DRV/r) in treatment-experienced patients with no DRV resistance-associated mutations (RAMs) at screening... CONCLUSION: Once-daily DRV/r 800/100 mg was noninferior in virologic response to twice-daily DRV/r 600/100 mg at 48 weeks in treatment-experienced patients with no DRV RAMs, and with a more favorable lipid profile. These findings support use of once-daily DRV/r in this population.
The effect of lopinavir/ritonavir and darunavir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants. [2011.02]
S/GSK1349572 is an unboosted, once-daily integrase inhibitor with a novel resistance profile. As standard of care for patients infected with HIV is combination therapy, the potential interaction between S/GSK1349572 and ritonavir-boosted protease inhibitors was evaluated... The most frequent drug-related AEs were diarrhea, dizziness, and headache.
Clinical Trials Related to Prezista (Darunavir)
TMC114-C202: A Study of Safety, Efficacy, and Tolerability of TMC114 and Low Dose Ritonavir in HIV-1 Infected Patients [Completed]
The purpose of this study is to determine the effectiveness, safety, and tolerability (how
well the body stands the drug) of an investigational protease inhibitor (PI) called TMC114
given with low dose ritonavir.
GRACE: A Study to Compare the Effectiveness, Safety and Tolerability of PREZISTA (Darunavir)/Ritonavir by Gender and Race When Administered With Other Antiretroviral Medications in Human Immunodeficiency Virus (HIV) Positive Women and Men. [Active, not recruiting]
The purpose of this study is to evaluate any differences in the effectiveness, safety, and
tolerability of PREZISTA (darunavir) 600 mg, administered with ritonavir 100 mg twice a day
on virologic response (defined as a viral load of < 50 copies/mL) over a 48-week treatment
period in HIV-positive women and men. Additional antiretroviral agents will also be
administered and will be chosen by the Investigator based on resistance testing and prior
treatment history (referred to as the Optimized Background Regimen (OBR)).
TMC114-C213: A Phase II Randomized, Controlled, Partially Blinded Trial to Investigate Dose-Response of TMC114/RTV in 3-Class-Experienced HIV-1 Infected Patients, Followed by an Open-Label Period on the Recommended Dose of TMC114/RTV. [Completed]
The purpose of this study is to determine the antiviral activity, safety and tolerability of
TMC114, formulated as an oral tablet, and administered with a low dose of ritonavir
A Pediatric Trial to Provide Dose Recommendation of TMC114/Rtv in HIV-1 Infected Children and Adolescents [Active, not recruiting]
The purpose of this study is to evaluate pharmacokinetics, short-term safety, tolerability
and antiviral activity to support dose recommendations of TMC114 administered in combination
with low-dose ritonavir and other antiretroviral (ARV) agents in treatment-experienced, HIV-1
infected pediatric patients aged from 6-17 years.
TMC114-C227: A Study to Evaluate the Effectiveness and Safety of TMC114 (Darunavir) With a Low Dose of Ritonavir as Monotherapy (no Other Anti-HIV Drugs Will be Given) in Patients Who Have Never Been Treated With Antiretrovirals (Anti-HIV Drugs) Previously [Terminated]
This is an open label study (no placebos are used; all patients will receive the true
medication) to evaluate the effectiveness of TMC114/rtv in treatment naïve (never previously
received anti-HIV drugs), HIV 1 infected patients.
Reports of Suspected Prezista (Darunavir) Side Effects
Maternal Exposure During Pregnancy (33),
Foetal Exposure During Pregnancy (20),
Abortion Spontaneous (16),
Renal Failure Acute (14),
Premature Baby (14),
Foetal Growth Restriction (13),
Gamma-Glutamyltransferase Increased (12), more >>
Page last updated: 2011-12-09