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The clinical pharmacology of integrase inhibitors

Expert Review of Clinical Pharmacology, 2018
Introduction: Treatment of HIV infection has consistently evolved in the last three decades. A steady improvement in efficacy tolerability, safety, and practical aspects of treatment intake has made HIV infection much easier to manage over the long term, and in optimal treatment conditions the life expectancy of persons living with HIV infection now ...
Giovanni, Di Perri   +3 more
openaire   +2 more sources

Integrase Strand Transfer Inhibitor Resistance in Integrase Strand Transfer Inhibitor-Naive Persons

AIDS Research and Human Retroviruses, 2021
There has been no systematic review of the prevalence of transmitted integrase strand transfer inhibitor (INSTI) resistance. We systematically searched the English-language PubMed database and GenBank to identify studies published since 2010 reporting 50 or more INSTI-naive HIV-1-infected adults undergoing integrase genotyping.
Alexander J, Bailey   +2 more
openaire   +2 more sources

Resistance to HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
HIV integrase inhibitors are potent antiretroviral drugs that efficiently decrease viral load in patients. Emergence of resistance mutations against this new class of drugs represents a threat to their long-term efficacy. The purpose of this review is to provide new information about the most recent mutations identified and other mutations that confer ...
Thibault, Mesplède   +2 more
openaire   +2 more sources

Tolerability of HIV integrase inhibitors

Current Opinion in HIV and AIDS, 2012
This review discusses the available safety data for three integrase strand transfer inhibitors (INSTIs)--raltegravir, elvitegravir and dolutegravir--derived from studies in both HIV-infected and HIV-uninfected cohorts.Phase 2 and 3 clinical trials show that all three INSTIs are well tolerated in treatment-naive and treatment-experienced patients with ...
Frederick J, Lee, Andrew, Carr
openaire   +2 more sources

Inhibitors of Human Immunodeficiency Virus Integrase

1999
Integration of the viral DNA into a host cell chromosome is an essential step for HIV replication and maintenance of persistent infection. Two viral factors are essential for integration: the viral DNA termini (the att sites) and IN. Accruing knowledge of the IN structure, catalytic mechanisms, and interactions with other proteins can be used to design
Y, Pommier, N, Neamati
openaire   +2 more sources

The future of integrase inhibitors of HIV-1

Current Opinion in Virology, 2012
Integration of the HIV-1 DNA is required and essential to maintain the viral DNA in the infected cell. Integration process occurs in several events, mainly endonucleolytic processing of the 3' ends of the viral DNA and strand transfer or joining of the viral and cellular DNA.
Isabelle, Malet   +2 more
openaire   +2 more sources

Quinoline-based HIV Integrase Inhibitors

Current Pharmaceutical Design, 2013
HIV integrase became an important target for drug development more than twenty years ago. However, progress has been hampered by the lack of assays suitable for high throughput screening, a reliable crystal structure or pharmacophore. Thus, a real breakthrough was only observed in 2007 with the introduction of the first integrase inhibitor, raltegravir,
openaire   +2 more sources

Next-Generation Integrase Inhibitors

Drugs, 2013
The integrase enzyme facilitates the incorporation of HIV-1 proviral DNA into the host cell genome and catalyses a function vital to viral replication. Inhibitors of this enzyme represent the newest class of antiretroviral drugs in our armamentarium to treat HIV-1 infection.
Sharon L, Karmon, Martin, Markowitz
openaire   +2 more sources

Development of Integrase Inhibitors for Treatment of AIDS: An Overview.

ChemInform, 2007
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Sonal, Dubey   +2 more
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HIV INTEGRASE INHIBITORS

2022
HIV infection is incredibly detrimental and fatal to people. Unfortunately, despite recent advancements and medications, it has not yet been completely eradicated. Opportunistic infections are added to the list of disorders in AIDS (Acquired Immune Deficiency Syndrome), an infectious disease that develops as a result of an impaired immune system.
openaire   +1 more source

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