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Etravirine

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1. Drug repositioning screening identifies etravirine as a potential therapeutic for friedreich's ataxia. (PubMed)

Drug repositioning screening identifies etravirine as a potential therapeutic for friedreich's ataxia. Friedreich's ataxia is an autosomal-recessive cerebellar ataxia caused by mutation of the frataxin gene, resulting in decreased frataxin expression, mitochondrial dysfunction, and oxidative stress. Currently, no treatment is available for Friedreich's ataxia patients. Given that levels of residual frataxin critically affect disease severity, the main goal of a specific therapy for Friedreich's (...) focused our attention on etravirine, an antiviral drug currently in use as an anti-human immunodeficiency virus therapy. Here, we show that etravirine can promote a significant increase in frataxin levels in cells derived from Friedreich's ataxia patients, by enhancing frataxin messenger RNA translation. Importantly, frataxin accumulation in treated patient cell lines is comparable to frataxin levels in unaffected carrier cells, suggesting that etravirine could be therapeutically relevant. Indeed

2019 Movement Disorders

2. Lack of a Clinically Significant Pharmacokinetic Interaction between Etravirine and Raltegravir Using an Original Approach Based on Drug Metabolism, Protein Binding, and Penetration in Seminal Fluid: A Pharmacokinetic Substudy of the ANRS-163 ETRAL Study. (PubMed)

Lack of a Clinically Significant Pharmacokinetic Interaction between Etravirine and Raltegravir Using an Original Approach Based on Drug Metabolism, Protein Binding, and Penetration in Seminal Fluid: A Pharmacokinetic Substudy of the ANRS-163 ETRAL Study. The ANRS163-ETRAL study showed that etravirine 200 mg/raltegravir 400 mg twice-daily dual therapy was highly effective in the treatment of human immunodeficiency virus (HIV)-infected patients older than age 45 years, with virologic (...) and therapeutic success rates at week 48 of 99.4% and 94.5%, respectively. The objective of this study was to determine whether a clinically significant pharmacokinetic interaction between etravirine and raltegravir exists by assessing steady-state total and unbound etravirine, raltegravir, and inactive raltegravir-glucuronide concentrations 12 hours after last intake (C12h ) in blood plasma (BP) and seminal plasma (SP).Pharmacokinetic analysis of data from the ANRS163-ETRAL study.One hundred forty-six HIV-1

2019 Pharmacotherapy

3. Etravirine (Intelence®)

Etravirine (Intelence®) Etravirine (Intelence®) Etravirine (Intelence®) All Wales Medicines Strategy Group (AWMSG) Record Status This is a bibliographic record of a published health technology assessment. No evaluation of the quality of this assessment has been made for the HTA database. Citation All Wales Medicines Strategy Group (AWMSG). Etravirine (Intelence®) Penarth: All Wales Therapeutics and Toxicology Centre (AWTTC), secretariat of the All Wales Medicines Strategy Group (AWMSG). AWMSG (...) Secretariat Assessment Report Advice No. 1683. 2013 Authors' conclusions Etravirine (Intelence®) is recommended as an option for use within NHS Wales, in combination with a boosted protease inhibitor and other antiretroviral medicinal products, for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced paediatric patients from 6 years to less than 18 years of age. Final publication URL Indexing Status Subject indexing assigned by CRD MeSH Child; HIV

2014 Health Technology Assessment (HTA) Database.

4. Impact of etravirine on hospitalization rate between 2005 and 2011 among heavily treated HIV-1-infected individuals on failing regimens. (PubMed)

Impact of etravirine on hospitalization rate between 2005 and 2011 among heavily treated HIV-1-infected individuals on failing regimens. Etravirine (ETR), a non-nucleoside reverse transcriptase inhibitor (NNRTI) available in France since 2006, is indicated for antiretroviral-experienced HIV-infected adults, in combination with a ritonavir-boosted protease inhibitor (PI). To assess its clinical impact in routine care, we compared hospitalization rates according to ETR + PI prescription

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2018 BMC Infectious Diseases

5. Optimizing concentrations of concomitant antiretrovirals by reducing etravirine doses: two case reports of complex drug-drug interactions. (PubMed)

Optimizing concentrations of concomitant antiretrovirals by reducing etravirine doses: two case reports of complex drug-drug interactions. We report the cases of two treatment-experienced HIV-infected patients with complex antiretroviral regimens that showed significant drug-drug interactions with etravirine. Unexpectedly high etravirine concentrations likely caused subtherapeutic levels of darunavir, elvitegravir and dolutegravir through concentration-dependent metabolic induction. Therapeutic (...) drug monitoring allowed safe etravirine dose decreases to manage these interactions.

2018 Antiviral Therapy

6. The HIV-1 reverse transcriptase E138A natural polymorphism decreases the genetic barrier to resistance to etravirine in vitro. (PubMed)

The HIV-1 reverse transcriptase E138A natural polymorphism decreases the genetic barrier to resistance to etravirine in vitro. The HIV-1 reverse transcriptase (RT) natural polymorphism E138A is included among the mutations with a minor impact on response to etravirine. However, the interpretation of E138A on etravirine susceptibility is not consistent across different genotypic resistance algorithms. The aim of the study was to investigate the effect of E138A on the genetic barrier (...) to resistance to etravirine in vitro.A panel of 20 clinically derived recombinant viruses (10 with WT 138E and 10 with 138A, all without any other resistance mutation) were cultured in the presence of increasing etravirine concentrations and analysed for genotypic changes at virus breakthrough. Parallel experiments were conducted with 138E/A/G/K/Q NL4-3-based clones.In the NL4-3 background, codon 138 changes increased etravirine resistance in the following order: Q > K > A > G > E. The 138A viruses were

2018 Journal of Antimicrobial Chemotherapy

7. Characteristics of Treatment-Experienced HIV-infected African Children and Adolescents Initiating Darunavir and/or Etravirine-based Antiretroviral Treatment. (PubMed)

Characteristics of Treatment-Experienced HIV-infected African Children and Adolescents Initiating Darunavir and/or Etravirine-based Antiretroviral Treatment. Data are limited on the selection and sequencing of second-line and third-line pediatric antiretroviral treatment (ART) in resource-limited settings. This study aimed to evaluate characteristics of African pediatric patients initiated on darunavir (DRV) and/or etravirine (ETR) through a specific drug donation program.This was a cross

2017 Pediatric Infectious Dsease Journal

8. Pharmacokinetics of darunavir/cobicistat and etravirine alone and co-administered in HIV-infected patients. (PubMed)

Pharmacokinetics of darunavir/cobicistat and etravirine alone and co-administered in HIV-infected patients. To determine the effect of etravirine on the pharmacokinetics of darunavir/cobicistat and vice versa. Safety and tolerability of this combination were also evaluated.Open-label, fixed-sequence trial in two cohorts of HIV-infected patients on therapy with darunavir/cobicistat 800/150 mg once daily (DRV cohort; n = 15) or etravirine 400 mg once daily (ETR cohort; n = 15). Etravirine (...) or darunavir/cobicistat were added on days 1-14 and 1-7 in participants in the DRV or ETR cohort, respectively. Full pharmacokinetic profiles were obtained on days 0 and 14 in the DRV cohort, and on days 0 and 7 in the ETR cohort. Darunavir, cobicistat and etravirine pharmacokinetic parameters [AUC0-24, Cmax and trough concentrations in plasma (C24)] were calculated for each individual by non-compartmental analysis and were compared using linear mixed-effects models. Adverse events and HIV-1 RNA in plasma

2017 Journal of Antimicrobial Chemotherapy

9. Interaction between Darunavir and Etravirine Is Partly Mediated by CYP3A5 Polymorphism. (PubMed)

Interaction between Darunavir and Etravirine Is Partly Mediated by CYP3A5 Polymorphism. To assess the impact of the loss-of-function CYP3A5*3 allele (rs776746, 6986A>G SNP) on darunavir (DRV) plasma concentrations.135 HIV-1 infected patients treated with DRV-based therapy were included in the study and plasma samples were obtained immediately before drug intake in order to determine DRV trough concentrations using an ultra performance liquid chromatography method (UPLC) with diode-array (...) detection (DAD). Noteworthy is the fact that in 16 (11.9%) patients, etravirine (ETR) was combined with DRV. CYP3A5 genotypes were determined using real time PCR method (TaqMan® genotyping assay). The patients were then classified into CYP3A5 expressors (CYP3A5*1 allele carriers) and non-expressors (CYP3A5*3 homozygous). Subsequently, the association between DRV plasma trough concentration ([DRV]plasma) and CYP3A5 genotype-based expression status was analyzed.45% of the patients were classified

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2016 PLoS ONE

10. Dual Therapy Etravirine + Raltegravir by Once Daily in HIV-positive Patients (ETRAL QD)

Dual Therapy Etravirine + Raltegravir by Once Daily in HIV-positive Patients (ETRAL QD) Dual Therapy Etravirine + Raltegravir by Once Daily in HIV-positive Patients (ETRAL QD) - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum number of saved studies (100). Please remove one or more studies (...) before adding more. Dual Therapy Etravirine + Raltegravir by Once Daily in HIV-positive Patients (ETRAL QD) (ETRALQD) The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. of clinical studies and talk to your health care provider before participating. Read our for details. ClinicalTrials.gov Identifier: NCT03369743 Recruitment Status : Recruiting First Posted

2017 Clinical Trials

11. Etravirine and Rilpivirine Drug Resistance Among HIV-1 Subtype C Infected Children Failing Non-Nucleoside Reverse Transcriptase Inhibitor-Based Regimens in South India (PubMed)

Etravirine and Rilpivirine Drug Resistance Among HIV-1 Subtype C Infected Children Failing Non-Nucleoside Reverse Transcriptase Inhibitor-Based Regimens in South India We have analyzed reverse transcriptase (RT) region of HIV-1 pol gene from 97 HIV-infected children who were identified as failing first-line therapy that included first-generation non-nucleoside RT inhibitors (Nevirapine and Efavirenz) for at least 6 months. We found that 54% and 65% of the children had genotypically predicted (...) resistance to second-generation non-nucleoside RT inhibitors drugs Etravirine (ETR) and Rilpivirine, respectively. These cross-resistance mutations may compromise future NNRTI-based regimens, especially in resource-limited settings. To complement these investigations, we also analyzed the sequences in Stanford database, Monogram weighted score, and DUET weighted score algorithms for ETR susceptibility and found almost perfect agreement between the three algorithms in predicting ETR susceptibility from

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2017 AIDS research and human retroviruses

12. Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial (PubMed)

Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial VIOLIN (TMC125IFD3002; NCT01422330) evaluated the safety, tolerability, and pharmacokinetics of etravirine with antiretrovirals other than darunavir/ritonavir in HIV-1-infected patients.In a 48-week, phase IV, single-arm, multicenter study, patients on prior antiretroviral therapy (⩾8 weeks) who needed to change regimen for virologic (...) failure (viral load ⩾ 500 copies/mL) or simplification/adverse events (viral load < 50 copies/mL) received etravirine 200 mg bid with ⩾1 other active antiretroviral, excluding darunavir/ritonavir or only nucleoside/tide reverse transcriptase inhibitors.Of 211 treated patients, 73% (n = 155) had baseline viral load ⩾ 50 copies/mL and 27% (n = 56) had baseline viral load < 50 copies/mL. Protease inhibitors were the most common background antiretrovirals (83%). Diarrhea was the most frequent adverse

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2017 SAGE open medicine

13. Pharmacokinetics of Darunavir/Ritonavir With Etravirine Both Twice Daily in Human Immunodeficiency Virus-Infected Adolescents and Young Adults (PubMed)

Pharmacokinetics of Darunavir/Ritonavir With Etravirine Both Twice Daily in Human Immunodeficiency Virus-Infected Adolescents and Young Adults Data on the combination of darunavir/ritonavir and etravirine both given twice daily in adolescents/young adults are lacking. In this study, we assessed the pharmacokinetics of darunavir/ritonavir 600/100 mg with etravirine 200 mg twice daily in 36 treatment-experienced human immunodeficiency virus-infected adolescents and young adults and found

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2017 Journal of the Pediatric Infectious Diseases Society

14. Efficacy of raltegravir, etravirine and darunavir/ritonavir for treatment-experienced HIV patients from a non-urban clinic population in the United States (PubMed)

Efficacy of raltegravir, etravirine and darunavir/ritonavir for treatment-experienced HIV patients from a non-urban clinic population in the United States The regimen of raltegravir (RAL), ritonavir-boosted darunavir (DAR/r), and etravirine (ETR) for HIV treatment-experienced patients in a non-clinical trial setting in the rural/semi-urban United States had not been evaluated.A retrospective cohort analysis was performed of adult patients prescribed the regimen from 2008 to 2013 at a HIV clinic

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2017 Therapeutic advances in infectious disease

15. Etravirine Pharmacokinetics in HIV-Infected Pregnant Women (PubMed)

Etravirine Pharmacokinetics in HIV-Infected Pregnant Women The study goal was to describe etravirine pharmacokinetics during pregnancy and postpartum in HIV-infected women.IMPAACT P1026s and PANNA are on-going, non-randomized, open-label, parallel-group, multi-center phase-IV prospective studies in HIV-infected pregnant women. Intensive steady-state 12-h pharmacokinetic profiles were performed from 2nd trimester through postpartum. Etravirine was measured at two labs using validated ultra (...) performance liquid chromatography (detection limits: 0.020 and 0.026 mcg/mL).Fifteen women took etravirine 200 mg twice-daily. Etravirine AUC0-12 was higher in the 3rd trimester compared to paired postpartum data by 34% (median 8.3 vs. 5.3 mcg*h/mL, p = 0.068). Etravirine apparent oral clearance was significantly lower in the 3rd trimester of pregnancy compared to paired postpartum data by 52% (median 24 vs. 38 L/h, p = 0.025). The median ratio of cord blood to maternal plasma concentration at delivery

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2016 Frontiers in pharmacology

16. Simultaneous Measurement of Etravirine, Maraviroc and Raltegravir in Pigtail Macaque Plasma, Vaginal Secretions and Vaginal Tissue using a LC-MS/MS Assay (PubMed)

Simultaneous Measurement of Etravirine, Maraviroc and Raltegravir in Pigtail Macaque Plasma, Vaginal Secretions and Vaginal Tissue using a LC-MS/MS Assay Etravirine (ETR), maraviroc (MVC) and raltegravir (RAL) are promising antiretroviral drugs being used in HIV treatment and may be interesting for prevention applications such as oral or topical pre-exposure prophylaxis. Here we describe a sensitive and accurate method for the simultaneous detection of ETR, MVC and RAL from pigtail macaque

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2016 Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

17. Role of Rilpivirine and Etravirine in Efavirenz and Nevirapine-Based Regimens Failure in a Resource-Limited Country: A Cross- Sectional Study (PubMed)

Role of Rilpivirine and Etravirine in Efavirenz and Nevirapine-Based Regimens Failure in a Resource-Limited Country: A Cross- Sectional Study Etravirine(ETR) can be used for patients who have failed NNRTI-based regimen. In Thailand, ETR is approximately 45 times more expensive than rilpivirine(RPV). However, there are no data of RPV use in NNRTI failure. Therefore, we assessed the susceptibility and mutation patterns of first line NNRTI failure and the possibility of using RPV compared to ETV

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2016 PloS one

18. Clinical Trial to Evaluate Drug-drug Interactions Between Darunavir/Cobicistat and Etravirine in Hiv- Infected Patients

Clinical Trial to Evaluate Drug-drug Interactions Between Darunavir/Cobicistat and Etravirine in Hiv- Infected Patients Clinical Trial to Evaluate Drug-drug Interactions Between Darunavir/Cobicistat and Etravirine in Hiv- Infected Patients - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum (...) number of saved studies (100). Please remove one or more studies before adding more. Clinical Trial to Evaluate Drug-drug Interactions Between Darunavir/Cobicistat and Etravirine in Hiv- Infected Patients The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our for details. ClinicalTrials.gov Identifier: NCT02818348 Recruitment Status : Completed First

2016 Clinical Trials

19. Etravirine inhibits ABCG2 drug transporter and affects transplacental passage of tenofovir disoproxil fumarate. (PubMed)

Etravirine inhibits ABCG2 drug transporter and affects transplacental passage of tenofovir disoproxil fumarate. All HIV positive pregnant women should receive combination antiretroviral therapy (cART) to prevent mother-to-child transmission (MTCT) of the virus. It has recently been shown that fetal exposure of nucleoside reverse transcriptase inhibitors (NRTIs) tenofovir disoproxil fumarate (TDF) and abacavir is decreased by placental ABC transporters p-glycoprotein (ABCB1) and BCRP (ABCG2 (...) ). The aim of this study was to evaluate transporter-mediated drug-drug interactions (DDI) between etravirine (TMC125), a novel non-nucleoside reverse transcriptase inhibitor used in cART, and the NRTIs and to assess the relevance of such DDI for transplacental pharmacokinetics of TDF and abacavir.In vitro accumulation assays and transport experiments on ABCB1 and ABCG2 overexpressing MDCKII monolayers were employed. Furthermore, the effect of etravirine on the transplacental passage of TDF and abacavir

2016 Placenta

20. Etravirine

Etravirine Etravirine Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Etravirine Etravirine Aka: Etravirine , Intelence From Related (...) "Etravirine." Click on the image (or right click) to open the source website in a new browser window. Related Studies (from Trip Database) Cost: Medications intelence (on 1/14/2017 at ) INTELENCE 100 MG TABLET $9.37 each INTELENCE 200 MG TABLET $18.94 each FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices

2018 FP Notebook

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