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Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals

BACKGROUND:: Tenofovir alafenamide (TAF), a prodrug of the nucleotide analogue tenofovir (TFV), is an antiretroviral (ARV) agent approved either as a complete regimen [elvitegravir/cobicistat/emtricitabine (F)/TAF, rilpivirine/F/TAF, bictegravir/F/TAF], or for use with other ARVs (F/TAF), for treatm... Full description

Journal Title: JAIDS Journal of Acquired Immune Deficiency Syndromes 2018, Vol.78(4), pp.465-472
Main Author: Begley, P., Rebecca
Other Authors: Das, M., Moupali , Zhong, M., Lijie , Ling, M., John , Kearney, M., Brian , Custodio, M., Joseph
Format: Electronic Article Electronic Article
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ID: ISSN: 1525-4135 ; DOI: 10.1097/QAI.0000000000001699
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recordid: ovid10.1097/QAI.0000000000001699
title: Pharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals
format: Article
creator:
  • Begley, P., Rebecca
  • Das, M., Moupali
  • Zhong, M., Lijie
  • Ling, M., John
  • Kearney, M., Brian
  • Custodio, M., Joseph
subjects:
  • Antiretroviral Drugs
  • Breast Cancer
  • Glycoproteins
  • ABC Transporters
  • Inhibitor Drugs
  • Cancer
  • Breast Cancer
  • Protein Transport
  • Ritonavir
  • Pharmacology
  • Lopinavir
  • Glycoprotein
  • Breast Cancer
  • Exposure
  • Antiviral Agents
  • Inducers
  • Tenofovir
  • Nucleotide Analogs
  • Drug Interaction
  • Proteins
  • Pharmacokinetics
  • Substrates
  • Pharmacokinetics
  • P-Glycoprotein
  • Exposure
  • Inhibitors
  • Antiretroviral Agents
  • Emtricitabine
  • Ritonavir
  • Inhibitors
  • Drug Interactions
  • Efavirenz
  • All Terrain Vehicles
  • Human Immunodeficiency Virus–HIV
ispartof: JAIDS Journal of Acquired Immune Deficiency Syndromes, 2018, Vol.78(4), pp.465-472
description: BACKGROUND:: Tenofovir alafenamide (TAF), a prodrug of the nucleotide analogue tenofovir (TFV), is an antiretroviral (ARV) agent approved either as a complete regimen [elvitegravir/cobicistat/emtricitabine (F)/TAF, rilpivirine/F/TAF, bictegravir/F/TAF], or for use with other ARVs (F/TAF), for treatment of HIV. TAF is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters. Disposition of TAF may be altered by comedications that can inhibit or induce P-gp or BCRP transporters. The effects of ARVs on the pharmacokinetics of TAF were evaluated in 3 studies. METHODS:: Healthy participants received TAF administered alone or with rilpivirine in study 1, with dolutegravir, ritonavir-boosted atazanavir (ATV + RTV), lopinavir (LPV/RTV), or darunavir (DRV + RTV) in study 2, and with the pharmacokinetic enhancer cobicistat or efavirenz in study 3. RESULTS:: Across the 3 studies, 98 participants received treatment with TAF and a coadministered agent (n = 10–34/cohort). All study treatments were well tolerated. TAF and TFV exposures were unaffected after co-administration with rilpivirine and dolutegravir. Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%–183% increases in TAF and 105%–316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%–24% decrease in TAF and TFV exposure. CONCLUSIONS:: Evaluation of the drug interaction between TAF and other commonly prescribed boosted and unboosted ARVs provides characterization of the susceptibility of TAF and/or TFV pharmacokinetics to inhibitors or inducers of P-gp/BCRP transporters.
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identifier: ISSN: 1525-4135 ; DOI: 10.1097/QAI.0000000000001699
fulltext: fulltext
issn:
  • 1525-4135
  • 15254135
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titlePharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals
creatorBegley, P., Rebecca ; Das, M., Moupali ; Zhong, M., Lijie ; Ling, M., John ; Kearney, M., Brian ; Custodio, M., Joseph
ispartofJAIDS Journal of Acquired Immune Deficiency Syndromes, 2018, Vol.78(4), pp.465-472
identifierISSN: 1525-4135 ; DOI: 10.1097/QAI.0000000000001699
descriptionBACKGROUND:: Tenofovir alafenamide (TAF), a prodrug of the nucleotide analogue tenofovir (TFV), is an antiretroviral (ARV) agent approved either as a complete regimen [elvitegravir/cobicistat/emtricitabine (F)/TAF, rilpivirine/F/TAF, bictegravir/F/TAF], or for use with other ARVs (F/TAF), for treatment of HIV. TAF is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters. Disposition of TAF may be altered by comedications that can inhibit or induce P-gp or BCRP transporters. The effects of ARVs on the pharmacokinetics of TAF were evaluated in 3 studies. METHODS:: Healthy participants received TAF administered alone or with rilpivirine in study 1, with dolutegravir, ritonavir-boosted atazanavir (ATV + RTV), lopinavir (LPV/RTV), or darunavir (DRV + RTV) in study 2, and with the pharmacokinetic enhancer cobicistat or efavirenz in study 3. RESULTS:: Across the 3 studies, 98 participants received treatment with TAF and a coadministered agent (n = 10–34/cohort). All study treatments were well tolerated. TAF and TFV exposures were unaffected after co-administration with rilpivirine and dolutegravir. Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%–183% increases in TAF and 105%–316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%–24% decrease in TAF and TFV exposure. CONCLUSIONS:: Evaluation of the drug interaction between TAF and other commonly prescribed boosted and unboosted ARVs provides characterization of the susceptibility of TAF and/or TFV pharmacokinetics to inhibitors or inducers of P-gp/BCRP transporters.
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subjectAntiretroviral Drugs ; Breast Cancer ; Glycoproteins ; ABC Transporters ; Inhibitor Drugs ; Cancer ; Breast Cancer ; Protein Transport ; Ritonavir ; Pharmacology ; Lopinavir ; Glycoprotein ; Breast Cancer ; Exposure ; Antiviral Agents ; Inducers ; Tenofovir ; Nucleotide Analogs ; Drug Interaction ; Proteins ; Pharmacokinetics ; Substrates ; Pharmacokinetics ; P-Glycoprotein ; Exposure ; Inhibitors ; Antiretroviral Agents ; Emtricitabine ; Ritonavir ; Inhibitors ; Drug Interactions ; Efavirenz ; All Terrain Vehicles ; Human Immunodeficiency Virus–HIV;
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titlePharmacokinetics of Tenofovir Alafenamide When Coadministered With Other HIV Antiretrovirals
descriptionBACKGROUND:: Tenofovir alafenamide (TAF), a prodrug of the nucleotide analogue tenofovir (TFV), is an antiretroviral (ARV) agent approved either as a complete regimen [elvitegravir/cobicistat/emtricitabine (F)/TAF, rilpivirine/F/TAF, bictegravir/F/TAF], or for use with other ARVs (F/TAF), for treatment of HIV. TAF is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters. Disposition of TAF may be altered by comedications that can inhibit or induce P-gp or BCRP transporters. The effects of ARVs on the pharmacokinetics of TAF were evaluated in 3 studies. METHODS:: Healthy participants received TAF administered alone or with rilpivirine in study 1, with dolutegravir, ritonavir-boosted atazanavir (ATV + RTV), lopinavir (LPV/RTV), or darunavir (DRV + RTV) in study 2, and with the pharmacokinetic enhancer cobicistat or efavirenz in study 3. RESULTS:: Across the 3 studies, 98 participants received treatment with TAF and a coadministered agent (n = 10–34/cohort). All study treatments were well tolerated. TAF and TFV exposures were unaffected after co-administration with rilpivirine and dolutegravir. Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%–183% increases in TAF and 105%–316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%–24% decrease in TAF and TFV exposure. CONCLUSIONS:: Evaluation of the drug interaction between TAF and other commonly prescribed boosted and unboosted ARVs provides characterization of the susceptibility of TAF and/or TFV pharmacokinetics to inhibitors or inducers of P-gp/BCRP transporters.
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1Copyright © 2018 Wolters Kluwer Health, Inc. All rights reserved.
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abstractBACKGROUND:: Tenofovir alafenamide (TAF), a prodrug of the nucleotide analogue tenofovir (TFV), is an antiretroviral (ARV) agent approved either as a complete regimen [elvitegravir/cobicistat/emtricitabine (F)/TAF, rilpivirine/F/TAF, bictegravir/F/TAF], or for use with other ARVs (F/TAF), for treatment of HIV. TAF is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) transporters. Disposition of TAF may be altered by comedications that can inhibit or induce P-gp or BCRP transporters. The effects of ARVs on the pharmacokinetics of TAF were evaluated in 3 studies. METHODS:: Healthy participants received TAF administered alone or with rilpivirine in study 1, with dolutegravir, ritonavir-boosted atazanavir (ATV + RTV), lopinavir (LPV/RTV), or darunavir (DRV + RTV) in study 2, and with the pharmacokinetic enhancer cobicistat or efavirenz in study 3. RESULTS:: Across the 3 studies, 98 participants received treatment with TAF and a coadministered agent (n = 10–34/cohort). All study treatments were well tolerated. TAF and TFV exposures were unaffected after co-administration with rilpivirine and dolutegravir. Coadministration with P-gp/BCRP inhibitors such as cobicistat or PI-based regimens (ATV + RTV, LPV/r, or DRV + RTV) resulted in a range of 6%–183% increases in TAF and 105%–316% increases in TFV exposure, whereas coadministration with a P-gp inducer, efavirenz, resulted in a 15%–24% decrease in TAF and TFV exposure. CONCLUSIONS:: Evaluation of the drug interaction between TAF and other commonly prescribed boosted and unboosted ARVs provides characterization of the susceptibility of TAF and/or TFV pharmacokinetics to inhibitors or inducers of P-gp/BCRP transporters.
pubCopyright © 2018 Wolters Kluwer Health, Inc. All rights reserved.
doi10.1097/QAI.0000000000001699
eissn19447884
date2018-08