Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial

Madruga, José Valdez; Cahn, Pedro; Grinsztejn, Beatriz; Haubrich, Richard; Lalezari, Jacob; Mills, Anthony; Pialoux, Gilles; Wilkin, Timothy; Peeters, Monika; Vingerhoets, Johan; Smedt, Goedele De; Leopold, Lorant; Trefiglio, Roberta; Woodfall, Brian

doi:10.1016/s0140-6736(07)61047-2

Cited by 438 publications

(353 citation statements)

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“…The results of the 48-week analysis also demonstrate a significant clinical benefit accompanying virologic suppression, with fewer individuals in the etravirine arm demonstrating new AIDS-defining illnesses or death, an outcome that was not statistically different between arms at week 24 [2].…”

Section: Significance Of the Resultsmentioning

confidence: 82%

“…The pooled 48-week analysis of the DUET (TMC125 to Demonstrate Undetectable viral load in patients Experienced with antretroviral Therapy)-1 and -2 studies designed to compare etravirine with placebo in combination with a darunavir/ ritonavir-containing optimized background regimens has updated the preliminary 24-week data from both trials [1][2][3]. Treatment goals in treatment-experienced HIV-infected patients remain similar to that of treatment-naive patients, with a target of virologic suppression (plasma viral load <50 copies/ml) [4].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Etravirine in combination with darunavir/ritonavir and optimized background regimen results in suppression of HIV replication in treatment-experienced patients

Hull

Montaner²

2010

Expert Opinion on Pharmacotherapy

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Section: Significance Of the Resultsmentioning

confidence: 82%

Section: Introductionmentioning

confidence: 99%

Etravirine in combination with darunavir/ritonavir and optimized background regimen results in suppression of HIV replication in treatment-experienced patients

Hull

Montaner²

2010

Expert Opinion on Pharmacotherapy

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“…They thus prevent the HIV protease from carrying out its normal function, which is the proteolytic processing of precursor viral proteins into mature viral proteins. The ten PIs presently available for the treatment of HIV infections are saquinavir, ritonavir, indinavir, nelfinavir, amprenavir, lopinavir, atazanavir, fosamprenavir, tipranavir and darunavir (Madruga et al, 2007;Lazzarin et al, 2007).…”

Section: Protease Inhibitors (Pis)mentioning

confidence: 99%

Twenty-six years of HIV science: an overview of anti-HIV drugs metabolism

Andrade

Freitas

Oliveira

2011

Braz. J. Pharm. Sci.

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From the identification of HIV as the agent causing AIDS, to the development of effective antiretroviral drugs, the scientific achievements in HIV research over the past twenty-six years have been formidable. Currently, there are twenty-five anti-HIV compounds which have been formally approved for clinical use in the treatment of AIDS. These compounds fall into six categories: nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), cell entry inhibitors or fusion inhibitors (FIs), co-receptor inhibitors (CRIs), and integrase inhibitors (INIs). Metabolism by the host organism is one of the most important determinants of the pharmacokinetic profile of a drug. Formation of active or toxic metabolites will also have an impact on the pharmacological and toxicological outcomes. Therefore, it is widely recognized that metabolism studies of a new chemical entity need to be addressed early in the drug discovery process. This paper describes an overview of the metabolism of currently available anti-HIV drugs.Uniterms: AIDS/treatment. Drugs/anti-HIV. Drugs/metabolism. Antiretroviral drugs. Biotransformation.Da identificação do HIV como o agente causador da AIDS, ao desenvolvimento de fármacos antirretrovirais eficazes, os avanços científicos na pesquisa sobre o HIV nos últimos vinte e seis anos foram marcantes. Atualmente, existem vinte e cinco fármacos anti-HIV formalmente aprovados pelo FDA para utilização clínica no tratamento da AIDS. Estes compostos são divididos em seis classes: inibidores nucleosídeos de transcriptase reversa (INTR), inibidores nucleotídeos de transcriptase reversa (INtTR), inibidores não-nucleosídeos de transcriptase reversa (INNTR), inibidores de protease (IP), inibidores da entrada celular ou inibidores de fusão (IF), inibidores de co-receptores (ICR) e inibidores de integrase (INI). O metabolismo consiste em um dos maiores determinantes do perfil farmacocinético de um fármaco. A formação de metabólitos ativos ou tóxicos terá impacto nas respostas farmacológicas ou toxicológicas do fármaco. Portanto, é amplamente reconhecido que estudos do metabolismo de uma nova entidade química devem ser realizados durante as fases iniciais do processo de desenvolvimento de fármacos. Este artigo descreve uma abordagem do metabolismo dos fármacos anti-HIV atualmente disponíveis na terapêutica.Unitermos: AIDS/tratamento. Fármacos/anti-HIV. Fármacos/antirretrovirais. Fármacos/metabolismo. Biotransformação. INTRODUCTIONThe human immunodeficiency virus (HIV) has been established as the causative agent of the acquired immunodeficiency syndrome (AIDS) for over twentysix years now (Barré-Sinoussi et al., 1983). During this time, an unprecedented success has been achieved in discovering anti-HIV drugs as reflected by the fact that there are now more drugs approved for the treatment of HIV than for all other viral infections put together (Mehellou, De Clercq, 2009). Despite this progress...

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“…(Lazzarin, et al, 2007;Madruga, et al, 2007) Etravirine was associated with superior virologic suppression compared with placebo, with up to 62% of patients in the etravirine group achieving undetectable viral loads, compared with 44% in the placebo group. (Lazzarin, et al, 2007;Madruga, et al, 2007) Etravirine exhibits retained activity despite multiple NNRTI mutations, with high rates of sustained efficacy at 48 weeks in heavily treatment-experienced patients. (Haubrich, et al, Abstract #790, CROI 2008;Johnson M, et al, Abstract #792, CROI, 2008) The tolerability profile is comparable to placebo, with the exception of a rash.…”

Section: New Non-nrtimentioning

confidence: 99%