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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 ...
Di Perri, Giovanni   +3 more
openaire   +2 more sources

Novel integrase inhibitors for HIV

Expert Opinion on Investigational Drugs, 2010
Integrase inhibitors are the newest class of antiretroviral agents developed to treat HIV-1 infection. Raltegravir (RAL), the only integrase inhibitor (INI) currently approved for the treatment of HIV-infected patients, has proven to be a potent and well-tolerated antiretroviral (ARV) agent.
Martin Markowitz, Nicole Prada
openaire   +3 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

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 ...
Peter K. Quashie   +2 more
openaire   +3 more sources

ChemInform Abstract: Potential Inhibitors of HIV Integrase

ChemInform, 1999
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Vasu Nair, Christophe Mathe
openaire   +3 more sources

Thiazolothiazepine Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1999
A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentatomic moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one
NEAMATI N.   +12 more
openaire   +5 more sources

Primary resistance to integrase inhibitors in Shenzhen

Journal of Antimicrobial Chemotherapy, 2022
Abstract Objectives In recent years, integrase strand transfer inhibitor (INSTI)-containing regimens have been increasingly adopted in treatment for HIV/AIDS and promoted as non-occupational post-exposure prophylaxis in China.
Yue Zhu   +16 more
openaire   +2 more sources

The Hunt for HIV-1 Integrase Inhibitors

AIDS Patient Care and STDs, 2006
Currently, there are three distinct mechanistic classes of antiretrovirals: inhibitors of the HIV- 1 reverse transcriptase and protease enzymes and inhibitors of HIV entry, including receptor and coreceptor binding and cell fusion. A new drug class that inhibits the HIV-1 integrase enzyme (IN) is in development and may soon be available in the clinic ...
Michael J. Kozal, Max Lataillade
openaire   +2 more sources

Raltegravir: The first HIV integrase inhibitor

Clinical Therapeutics, 2008
The availability of new classes of antiretroviral drugs has made it possible for HIV-infected individuals who are highly treatment experienced to achieve the goals of immunologic recovery and virologic suppression. Raltegravir is the first integrase inhibitor to be approved by the US Food and Drug Administration for use in antiretroviral treatment ...
Betty J. Dong, Jennifer Cocohoba
openaire   +3 more sources

Integrase inhibitors to treat HIV/Aids

Nature Reviews Drug Discovery, 2005
HIV integrase is a rational target for treating HIV infection and preventing AIDS. It took approximately 12 years to develop clinically usable inhibitors of integrase, and Phase I clinical trials of integrase inhibitors have just begun. This review focuses on the molecular basis and rationale for developing integrase inhibitors.
Allison A. Johnson   +2 more
openaire   +3 more sources

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