Results 261 to 270 of about 86,566 (299)

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
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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, Peter K, Quashie, Mark A, Wainberg   +2 more
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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.
Yves, Pommier, Allison A, Johnson, Christophe, Marchand   +2 more
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Coumarin-Based Inhibitors of HIV Integrase

Journal of Medicinal Chemistry, 1997
The structures of a large number of HIV-1 integrase inhibitors have in common two aryl units separated by a central linker. Frequently at least one of these aryl moieties must contain 1,2-dihydroxy substituents in order to exhibit high inhibitory potency.
H, Zhao, N, Neamati, H, Hong, A, Mazumder, S, Wang, S, Sunder, G W, Milne, Y, Pommier, T R, Burke   +8 more
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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 ...
Jennifer, Cocohoba, Betty J, Dong
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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., TURPIN J. A, WINSLOW H. E., CHRISTENSEN J. L., WILLIAMSON K., ORR A., RICE W. G., POMMIER Y., GAROFALO A., BRIZZI A., CAMPIANI G., FIORINI I., NACCI V.   +12 more
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Hydrazide-Containing Inhibitors of HIV-1 Integrase

Journal of Medicinal Chemistry, 1997
Inhibitors of HIV integrase are currently being sought as potential new therapeutics for the treatment of AIDS. A large number of inhibitors discovered to date contain the o-bis-hydroxy catechol structure. In an effort to discover structural leads for the development of new HIV integrase inhibitors which do not rely on this potentially cytotoxic ...
H, Zhao, N, Neamati, S, Sunder, H, Hong, S, Wang, G W, Milne, Y, Pommier, T R, Burke   +7 more
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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 ...
Max, Lataillade, Michael J, Kozal
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Integrase Inhibitors Against HIV: Efficacy and Resistance

Future Virology, 2016
Divisione Clinicizzata di Malattie Infettive, Dipartimento di Scienze Biomediche e Cliniche ‘Luigi Sacco’, Universita degli Studi di Milano, via G.B. Grassi 74, 20157 Milano, Italy *Author for correspondence: Tel.: +39 02 5031 9761; Fax: +39 02 5031 9758; stefano.rusconi@unimi ...
P. Tau, S. Rusconi
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Raltegravir: an integrase inhibitor for HIV-1

Expert Opinion on Investigational Drugs, 2008
The need to develop antiretroviral agents with novel mechanisms of action persists for the treatment of both antiretroviral- experienced and antiretroviral-naive patients with HIV/AIDS. This is mandated, in part, by the perpetual advent of antiretroviral-resistant HIV-1 strains.
Teresa H, Evering, Martin, Markowitz
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