Raltegravir in HIV-1 infection: Safety and Efficacy in Treatment-naïve Patients.

Raltegravir does not revert efflux activity of MDR1-P-glycoprotein in human MDR cells. BMC Pharmacol Toxicol (2013) 0.80

Combination antiretroviral therapy with raltegravir leads to rapid immunologic reconstitution in treatment-naive patients with chronic HIV infection. J Infect Dis (2013) 0.80

Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS. HIV AIDS (Auckl) (2014) 0.77

HIV population dynamics in vivo: implications for genetic variation, pathogenesis, and therapy. Science (1995) 18.40

Earlier versus later start of antiretroviral therapy in HIV-infected adults with tuberculosis. N Engl J Med (2011) 7.13

Residues critical for retroviral integrative recombination in a region that is highly conserved among retroviral/retrotransposon integrases and bacterial insertion sequence transposases. Mol Cell Biol (1992) 6.77

The genetic basis of the reduced expression of bilirubin UDP-glucuronosyltransferase 1 in Gilbert's syndrome. N Engl J Med (1995) 6.73

Timing of antiretroviral therapy for HIV-1 infection and tuberculosis. N Engl J Med (2011) 6.42

Identification of conserved amino acid residues critical for human immunodeficiency virus type 1 integrase function in vitro. J Virol (1992) 6.07

Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med (2008) 5.58

HIV-1 replication and immune dynamics are affected by raltegravir intensification of HAART-suppressed subjects. Nat Med (2010) 5.36

Integration of antiretroviral therapy with tuberculosis treatment. N Engl J Med (2011) 5.31

Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial. Lancet (2009) 5.00

Retroviral intasome assembly and inhibition of DNA strand transfer. Nature (2010) 4.99

Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr (2006) 4.71

Rapid and durable antiretroviral effect of the HIV-1 Integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study. J Acquir Immune Defic Syndr (2007) 4.67

Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov (2005) 4.46

Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes. Proc Natl Acad Sci U S A (2002) 3.40

The effect of raltegravir intensification on low-level residual viremia in HIV-infected patients on antiretroviral therapy: a randomized controlled trial. PLoS Med (2010) 3.24

A randomized, controlled trial of raltegravir intensification in antiretroviral-treated, HIV-infected patients with a suboptimal CD4+ T cell response. J Infect Dis (2011) 3.10

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem (2008) 3.09

HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. Proc Natl Acad Sci U S A (2000) 3.00

Effect of raltegravir-containing intensification on HIV burden and T-cell activation in multiple gut sites of HIV-positive adults on suppressive antiretroviral therapy. AIDS (2010) 2.94

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother (2010) 2.89

Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial. Lancet Infect Dis (2011) 2.66

Switch to a raltegravir-based regimen versus continuation of a lopinavir-ritonavir-based regimen in stable HIV-infected patients with suppressed viraemia (SWITCHMRK 1 and 2): two multicentre, double-blind, randomised controlled trials. Lancet (2010) 2.63

The core and carboxyl-terminal domains of the integrase protein of human immunodeficiency virus type 1 each contribute to nonspecific DNA binding. J Virol (1994) 2.56

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase. Proc Natl Acad Sci U S A (2004) 2.55

The DNA-binding domain of HIV-1 integrase has an SH3-like fold. Nat Struct Biol (1995) 2.53

Safety, tolerability, and pharmacokinetics of raltegravir after single and multiple doses in healthy subjects. Clin Pharmacol Ther (2007) 2.53

Short-course raltegravir intensification does not reduce persistent low-level viremia in patients with HIV-1 suppression during receipt of combination antiretroviral therapy. Clin Infect Dis (2010) 2.51

Zinc folds the N-terminal domain of HIV-1 integrase, promotes multimerization, and enhances catalytic activity. Proc Natl Acad Sci U S A (1996) 2.46

Raltegravir versus Efavirenz regimens in treatment-naive HIV-1-infected patients: 96-week efficacy, durability, subgroup, safety, and metabolic analyses. J Acquir Immune Defic Syndr (2010) 2.37

Efficacy of a nucleoside-sparing regimen of darunavir/ritonavir plus raltegravir in treatment-naive HIV-1-infected patients (ACTG A5262). AIDS (2011) 2.22

In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug Metab Dispos (2005) 2.19

Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the human immunodeficiency virus 1 integrase enzyme. Drug Metab Dispos (2007) 2.17

Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A (2010) 2.16

Functional and structural characterization of the integrase from the prototype foamy virus. Nucleic Acids Res (2008) 2.07

Sustained antiretroviral effect of raltegravir after 96 weeks of combination therapy in treatment-naive patients with HIV-1 infection. J Acquir Immune Defic Syndr (2009) 1.83

Induction of CYP3A4 by efavirenz in primary human hepatocytes: comparison with rifampin and phenobarbital. J Clin Pharmacol (2004) 1.79

Long-term treatment with raltegravir or efavirenz combined with tenofovir/emtricitabine for treatment-naive human immunodeficiency virus-1-infected patients: 156-week results from STARTMRK. Clin Infect Dis (2011) 1.77

Characterization and structural analysis of HIV-1 integrase conservation. AIDS Rev (2009) 1.76

Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes. Antimicrob Agents Chemother (2011) 1.68

The complexities of antiretroviral drug-drug interactions: role of ABC and SLC transporters. Trends Pharmacol Sci (2009) 1.62

Structure-based mutational analysis of the C-terminal DNA-binding domain of human immunodeficiency virus type 1 integrase: critical residues for protein oligomerization and DNA binding. J Virol (1998) 1.58

A pilot study of abacavir/lamivudine and raltegravir in antiretroviral-naïve HIV-1-infected patients: 48-week results of the SHIELD trial. HIV Clin Trials (2010) 1.55

Impact of Y143 HIV-1 integrase mutations on resistance to raltegravir in vitro and in vivo. Antimicrob Agents Chemother (2009) 1.50

No effect of raltegravir intensification on viral replication markers in the blood of HIV-1-infected patients receiving antiretroviral therapy. J Acquir Immune Defic Syndr (2012) 1.39

Substitution of raltegravir for ritonavir-boosted protease inhibitors in HIV-infected patients: the SPIRAL study. AIDS (2010) 1.39

Clinical pharmacology profile of raltegravir, an HIV-1 integrase strand transfer inhibitor. J Clin Pharmacol (2011) 1.38

Structural insights into the retroviral DNA integration apparatus. Curr Opin Struct Biol (2011) 1.36

Transmission of integrase strand-transfer inhibitor multidrug-resistant HIV-1: case report and response to raltegravir-containing antiretroviral therapy. Antivir Ther (2011) 1.34

Evolution of raltegravir resistance during therapy. J Antimicrob Chemother (2009) 1.33

Transmitted raltegravir resistance in an HIV-1 CRF_AG-infected patient. Antivir Ther (2011) 1.32

Selective-advantage profile of human immunodeficiency virus type 1 integrase mutants explains in vivo evolution of raltegravir resistance genotypes. J Virol (2009) 1.30

Inhibition of human immunodeficiency virus type 1 concerted integration by strand transfer inhibitors which recognize a transient structural intermediate. J Virol (2007) 1.30

Natural polymorphisms of human immunodeficiency virus type 1 integrase and inherent susceptibilities to a panel of integrase inhibitors. Antimicrob Agents Chemother (2009) 1.27

Evolution of integrase resistance during failure of integrase inhibitor-based antiretroviral therapy. J Acquir Immune Defic Syndr (2010) 1.24

Effect of rifampin, a potent inducer of drug-metabolizing enzymes, on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother (2009) 1.24

Effect of low-, moderate-, and high-fat meals on raltegravir pharmacokinetics. J Clin Pharmacol (2010) 1.22

Pharmacokinetics of raltegravir in individuals with UGT1A1 polymorphisms. Clin Pharmacol Ther (2009) 1.21

Molecular Interactions between HIV-1 integrase and the two viral DNA ends within the synaptic complex that mediates concerted integration. J Mol Biol (2009) 1.19

Patterns of resistance development with integrase inhibitors in HIV. Infect Drug Resist (2011) 1.17

Longitudinal analysis of raltegravir susceptibility and integrase replication capacity of human immunodeficiency virus type 1 during virologic failure. Antimicrob Agents Chemother (2009) 1.16

Raltegravir treatment intensification does not alter cerebrospinal fluid HIV-1 infection or immunoactivation in subjects on suppressive therapy. J Infect Dis (2011) 1.15

Cross-resistance profile of the novel integrase inhibitor Dolutegravir (S/GSK1349572) using clonal viral variants selected in patients failing raltegravir. J Infect Dis (2011) 1.15

Switching between raltegravir resistance pathways analyzed by deep sequencing. AIDS (2011) 1.11

Cross-resistance profile determination of two second-generation HIV-1 integrase inhibitors using a panel of recombinant viruses derived from raltegravir-treated clinical isolates. Antimicrob Agents Chemother (2010) 1.08

Early emergence of raltegravir resistance mutations in patients receiving HAART salvage regimens. J Med Virol (2010) 1.08

Elite controllers as a model of functional cure. Curr Opin HIV AIDS (2011) 1.06

The HIV-1 integrase mutations Y143C/R are an alternative pathway for resistance to Raltegravir and impact the enzyme functions. PLoS One (2010) 1.04

Genotypic/phenotypic patterns of HIV-1 integrase resistance to raltegravir. J Antimicrob Chemother (2010) 1.04

Elvitegravir: a new HIV integrase inhibitor. Antivir Chem Chemother (2009) 1.01

Physical trapping of HIV-1 synaptic complex by different structural classes of integrase strand transfer inhibitors. Biochemistry (2010) 0.96

Long-term safety from the raltegravir clinical development program. Curr HIV Res (2011) 0.91

Management of HIV infection in treatment-naive patients: a review of the most current recommendations. Am J Health Syst Pharm (2011) 0.91

A randomized cross-over study to compare raltegravir and efavirenz (SWITCH-ER study). AIDS (2011) 0.90

Efficacy and safety of raltegravir in treatment-experienced HIV-1-infected patients switching from enfuvirtide-based regimens: 48 week results of the randomized EASIER ANRS 138 trial. J Antimicrob Chemother (2011) 0.87

HIV-1 Integrase Strand Transfer Inhibitors: Novel Insights into their Mechanism of Action. Retrovirology (Auckl) (2008) 0.86

Lopinavir/Ritonavir: a review of its use in the management of HIV-1 infection. Drugs (2010) 0.84

Clinical efficacy of raltegravir against B and non-B subtype HIV-1 in phase III clinical studies. AIDS (2011) 0.84

Clinical experience of raltegravir-containing regimens in HIV-infected patients during rifampicin-containing treatment of tuberculosis. J Antimicrob Chemother (2011) 0.83

Resistance to inhibitors of the human immunodeficiency virus type 1 integration. Braz J Infect Dis (2011) 0.83

HIV-1 integrase strand transfer inhibitors stabilize an integrase-single blunt-ended DNA complex. J Mol Biol (2011) 0.80

Postprandial lipid effects of low-dose ritonavir vs. raltegravir in HIV-uninfected adults. AIDS (2010) 0.79

Pharmacokinetics of double-dose raltegravir in two patients with HIV infection and tuberculosis. AIDS (2010) 0.78

Initial results reported on raltegravir once-daily dosing. AIDS Patient Care STDS (2011) 0.76