ArticleAntimicrobial agents and chemotherapy2009
Combination of tenofovir and emtricitabine plus efavirenz: in vitro modulation of ABC transporter and intracellular drug accumulation.
Article in Antimicrobial agents and chemotherapy, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 48 citations in OpenAlex.
- No evidence for induction of ABC transporters in peripheral blood mononuclear cells in humans after 14 days of efavirenz treatment.Antimicrobial agents and chemotherapy · 2010Trial
- Drug transporter mRNA expression and genital inflammation in South African women on oral pre-exposure prophylaxis (PrEP).AIDS research and therapy · 2025Article
- Efavirenz: History, Development and Future.Biomolecules · 2022Review
- Pharmacogenomics of drug transporters for antiretroviral long-acting pre-exposure prophylaxis for HIV.Frontiers in genetics · 2022Review
- Mathematical Modelling of the Molecular Mechanisms of Interaction of Tenofovir with Emtricitabine against HIV.Viruses · 2021Article
- The Lymphoid Tissue Pharmacokinetics of Tenofovir Disoproxil Fumarate and Tenofovir Alafenamide in HIV-Infected Persons.Clinical pharmacology and therapeutics · 2020Article
- Multiple Drug Transporters Contribute to the Placental Transfer of Emtricitabine.Antimicrobial agents and chemotherapy · 2019Article
- Polyanionic carbosilane dendrimers as a new adjuvant in combination with latency reversal agents for HIV treatment.Journal of nanobiotechnology · 2019Article
- Article
- Modified halloysite nanotubes reduce the toxic effects of zearalenone in gestating sows on growth and muscle development of their offsprings.Journal of animal science and biotechnology · 2016Article
- Expression of Genes for Drug Transporters in the Human Female Genital Tract and Modulatory Effect of Antiretroviral Drugs.PloS one · 2015Article
- The development and validation of a method using high-resolution mass spectrometry (HRMS) for the qualitative detection of antiretroviral agents in human blood.Clinica chimica acta; international journal of clinical chemistry · 2014Article
- Toxic effects of maternal zearalenone exposure on uterine capacity and fetal development in gestation rats.Reproductive sciences (Thousand Oaks, Calif.) · 2014Article
- Drug synergy of tenofovir and nanoparticle-based antiretrovirals for HIV prophylaxis.PloS one · 2013Article
- Susceptibility of juvenile and adult blood-brain barrier to endothelin-1: regulation of P-glycoprotein and breast cancer resistance protein expression and transport activity.Journal of neuroinflammation · 2012Article
- Mechanism of efavirenz influence on methadone pharmacokinetics and pharmacodynamics.Clinical pharmacology and therapeutics · 2012Article
- AtriplaR/anti-TB combination in TB/HIV patients. Drug in focus.BMC research notes · 2011Article
- Use of antineoplastic agents in patients with cancer who have HIV/AIDS.The Lancet. Oncology · 2011Review
- Influence of drug transport proteins on the pharmacokinetics and drug interactions of HIV protease inhibitors.Journal of pharmaceutical sciences · 2011Review
- Interactions of tenofovir, Lamivudine, abacavir and Didanosine in primary human cells.Pharmaceutics · 2011Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Efflux proteins have been shown to greatly affect the uptake of antiretroviral drugs by cells and to hamper their access to the human immunodeficiency virus type 1 replication site. This study evaluated the factors that may lead to drug-drug interactions between emtricitabine (FTC), tenofovir (TFV), and efavirenz (EFV), including the modulation of efflux transporter expression and function. Peripheral blood mononuclear cells from healthy volunteers were used to determine whether or not an interaction between antiretroviral drugs and target cells occurred in any combination of FTC, TFV, EFV, FTC-TFV, TFV-EFV, or FTC-TFV-EFV. Following 20 h of treatment, intracellular drug concentrations were measured by liquid chromatography-tandem mass spectrometry. Efflux transporter functionality and inhibitor drug properties were assessed by measuring fluorescent dye efflux. ABCB1 (P-glycoprotein), ABCC 1 to 6 (multidrug resistance-associated protein), and OAT (organic anion transporter) expression in response to the treatments was quantified by semiquantitative real-time PCR. Cells treated with a double combination (FTC-TFV or TFV-EFV) or the triple combination (FTC-TFV-EFV) produced higher FTC and TFV intracellular concentrations than cells treated with FTC or TFV alone. However, no change in the EFV intracellular concentration was observed. FTC tended to induce abcc5 mRNA expression and EFV tended to induce abcc1 and abcc6 mRNA expression, whereas TFV tended to reduce mdr1, abcc1, abcc5, and abcc6 mRNA expression. Under these conditions, a decrease in the functionality of ABCC was observed, and this decrease was associated with the direct inhibitory actions of these drugs. This in vitro study reveals a benefit of the combination FTC-TFV-EFV in terms of the intracellular FTC and TFV concentrations and highlights the pharmacological mechanisms that lead to this effect.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.