Overview of boosted protease inhibitors in treatment-experienced HIV-infected patients

Antiretroviral drug combinations that include two nucleoside reverse transcriptase inhibitors and a protease inhibitor (PI) can suppress HIV replication to undetectable levels, improving the prognosis of HIV-infected individuals. The aim of therapy is complete virological suppression, with a current...

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Veröffentlicht in:Journal of antimicrobial chemotherapy 2007-12, Vol.60 (6), p.1195-1205
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description Antiretroviral drug combinations that include two nucleoside reverse transcriptase inhibitors and a protease inhibitor (PI) can suppress HIV replication to undetectable levels, improving the prognosis of HIV-infected individuals. The aim of therapy is complete virological suppression, with a current goal of
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The aim of therapy is complete virological suppression, with a current goal of &lt;50 copies/mL HIV-1 RNA, in order to minimize the occurrence of drug resistance. Improved understanding of the pharmacology of PIs, primarily the importance of adequate drug exposure, has led to the widespread administration of PIs combined with a low ‘boosting’ dose of ritonavir. The combination of PIs with ritonavir can improve treatment responses in both treatment-naive and -experienced patients. Boosted PIs are an important therapeutic option for HIV and extensive data exist supporting their use. Use of individual agents should be guided by a resistance test at all stages of treatment from naive through to highly treatment-experienced patients. Currently, seven boosted PIs have both US and European licensing approval: indinavir, saquinavir, lopinavir, fosamprenavir, atazanavir, tipranavir and darunavir (formerly TMC114). The preferred first-line option in the USA is lopinavir. Many of the older PIs are less effective and/or have less favourable tolerability profiles. Emergent PI resistance is a major challenge in treatment, and it can be accelerated by partial suppression of viral load through inappropriate therapy combinations. Using the newer boosted PIs, which have more robust resistance profiles, with an optimized background regimen may increase the likelihood of complete viral suppression. This review discusses the relative strengths and weaknesses of boosted PIs in current practice.</description><identifier>ISSN: 0305-7453</identifier><identifier>EISSN: 1460-2091</identifier><identifier>DOI: 10.1093/jac/dkm364</identifier><identifier>PMID: 17890281</identifier><identifier>CODEN: JACHDX</identifier><language>eng</language><publisher>Oxford: Oxford University Press</publisher><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiretroviral drugs ; antiretroviral therapy ; antiviral ; Biological and medical sciences ; Biomedical research ; Drug Resistance, Viral - genetics ; Drug Therapy, Combination ; Europe ; HIV ; HIV Infections - drug therapy ; HIV Infections - virology ; HIV Protease - drug effects ; HIV Protease - genetics ; HIV Protease Inhibitors - administration &amp; dosage ; HIV Protease Inhibitors - classification ; HIV Protease Inhibitors - therapeutic use ; HIV-1 - drug effects ; HIV-1 - enzymology ; HIV-1 - genetics ; Human immunodeficiency virus ; Human immunodeficiency virus 1 ; Human viral diseases ; Humans ; Immunodeficiencies ; Immunodeficiencies. Immunoglobulinopathies ; Immunopathology ; Infectious diseases ; Medical prognosis ; Medical sciences ; Microbiology ; Pharmacology ; Pharmacology. 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Antiparasitic agents</subject><subject>Antiretroviral drugs</subject><subject>antiretroviral therapy</subject><subject>antiviral</subject><subject>Biological and medical sciences</subject><subject>Biomedical research</subject><subject>Drug Resistance, Viral - genetics</subject><subject>Drug Therapy, Combination</subject><subject>Europe</subject><subject>HIV</subject><subject>HIV Infections - drug therapy</subject><subject>HIV Infections - virology</subject><subject>HIV Protease - drug effects</subject><subject>HIV Protease - genetics</subject><subject>HIV Protease Inhibitors - administration &amp; dosage</subject><subject>HIV Protease Inhibitors - classification</subject><subject>HIV Protease Inhibitors - therapeutic use</subject><subject>HIV-1 - drug effects</subject><subject>HIV-1 - enzymology</subject><subject>HIV-1 - genetics</subject><subject>Human immunodeficiency virus</subject><subject>Human immunodeficiency virus 1</subject><subject>Human viral diseases</subject><subject>Humans</subject><subject>Immunodeficiencies</subject><subject>Immunodeficiencies. 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subjects Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiretroviral drugs
antiretroviral therapy
antiviral
Biological and medical sciences
Biomedical research
Drug Resistance, Viral - genetics
Drug Therapy, Combination
Europe
HIV
HIV Infections - drug therapy
HIV Infections - virology
HIV Protease - drug effects
HIV Protease - genetics
HIV Protease Inhibitors - administration & dosage
HIV Protease Inhibitors - classification
HIV Protease Inhibitors - therapeutic use
HIV-1 - drug effects
HIV-1 - enzymology
HIV-1 - genetics
Human immunodeficiency virus
Human immunodeficiency virus 1
Human viral diseases
Humans
Immunodeficiencies
Immunodeficiencies. Immunoglobulinopathies
Immunopathology
Infectious diseases
Medical prognosis
Medical sciences
Microbiology
Pharmacology
Pharmacology. Drug treatments
PIs
Protease inhibitors
Randomized Controlled Trials as Topic
Ritonavir - administration & dosage
Ritonavir - therapeutic use
Treatment Outcome
United States
Viral diseases
Viral diseases of the lymphoid tissue and the blood. Aids
title Overview of boosted protease inhibitors in treatment-experienced HIV-infected patients
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