ArticlePharmaceutical research2013
Role of drug efflux and uptake transporters in atazanavir intestinal permeability and drug-drug interactions.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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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.
The trial behind it
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
25 citing papers in PubMed, 69 citations in OpenAlex.
- Model-based evaluation of the interaction between ritonavir-boosted atazanavir and rifampicin in Ugandan adults with HIV.British journal of clinical pharmacology · 2025Trial
- Methotrexate Decreases Tenofovir Exposure in Antiretroviral-Suppressed Individuals Living With HIV.Journal of acquired immune deficiency syndromes (1999) · 2020Trial
- An Insectified Caco-2 Cell-Based Assay to Monitor Pesticide Transport Processes and Pharmacokinetics.International journal of molecular sciences · 2026Article
- Application of Physiologically Based Pharmacokinetic Modeling in the Research of Anti-HIV Drugs.Current drug metabolism · 2025Review
- The pH-dependence of efflux ratios determined with bidirectional transport assays across cellular monolayers.International journal of pharmaceutics: X · 2024Article
- Simplifying the Extended Clearance Concept Classification System (EC3S) to Guide Clearance Prediction in Drug Discovery.Pharmaceutical research · 2023Article
- Drug Interactions for Patients with Respiratory Diseases Receiving COVID-19 Emerged Treatments.International journal of environmental research and public health · 2021Review
- Disease-drug and drug-drug interaction in COVID-19: Risk and assessment.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2021Review
- Transport Properties of Statins by Organic Anion Transporting Polypeptide 1A2 and Regulation by Transforming Growth Factor-The Journal of pharmacology and experimental therapeutics · 2021Article
- An update on drug-drug interactions between antiretroviral therapies and drugs of abuse in HIV systems.Expert opinion on drug metabolism & toxicology · 2020Review
- HIV-1 Sanctuary Sites-the Role of Membrane-Associated Drug Transporters and Drug Metabolic Enzymes.The AAPS journal · 2020Review
- Anti-HIV and Anti-Hepatitis C Virus Drugs Inhibit P-Glycoprotein Efflux Activity in Caco-2 Cells and Precision-Cut Rat and Human Intestinal Slices.Antimicrobial agents and chemotherapy · 2019Article
- The Pre-clinical Toolbox of Pharmacokinetics and Pharmacodynamics:Frontiers in pharmacology · 2019Review
- PharmGKB summary: atazanavir pathway, pharmacokinetics/pharmacodynamics.Pharmacogenetics and genomics · 2018Article
- Effects of HIV-1 Tat and Methamphetamine on Blood-Brain Barrier Integrity and FunctionAntimicrobial agents and chemotherapy · 2017Article
- Cellular Models and In Vitro Assays for the Screening of modulators of P-gp, MRP1 and BCRP.Molecules (Basel, Switzerland) · 2017Review
- Dose- and Formulation-Dependent Non-Linear Pharmacokinetic Model of Paritaprevir, a Protease Inhibitor for the Treatment of Hepatitis C Virus Infection: Combined Analysis from 12 Phase I Studies.Clinical pharmacokinetics · 2016Article
- One-step self-assembled nanomicelles for improving the oral bioavailability of nimodipine.International journal of nanomedicine · 2016Article
- Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters.Antimicrobial agents and chemotherapy · 2015Article
- Drug-drug interactions between anti-retroviral therapies and drugs of abuse in HIV systems.Expert opinion on drug metabolism & toxicology · 2015Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the role of membrane-associated drug transporters in regulating the intestinal absorption of the HIV-1 protease inhibitor, atazanavir, and assess the potential contribution of these transporters in clinical interactions of atazanavir with other protease inhibitors and tenofovir disoproxil fumarate (TDF).
methodsIntestinal permeability of atazanavir was investigated in vitro, using the Caco-2 cell line system grown on Transwell inserts, and in situ, by single-pass perfusion of rat intestinal segments, jejunum and ileum, in the absence or presence of standard transporter inhibitors or antiretroviral drugs.
resultsAtazanavir accumulation by Caco-2 cells was susceptible to inhibition by P-glycoprotein and organic anion transporting polypeptide (OATP) family inhibitors and several antiretroviral drugs (protease inhibitors, TDF). The secretory flux of atazanavir (basolateral-to-apical Papp) was 11.7-fold higher than its absorptive flux. This efflux ratio was reduced to 1.5-1.7 in the presence of P-glycoprotein inhibitors or ritonavir. P-glycoprotein inhibition also resulted in 1.5-2.5-fold increase in atazanavir absorption in situ. Co-administration of TDF, however, reduced atazanavir intestinal permeability by 13-49%, similar to the effect observed clinically.
conclusionsDrug transporters such as P-glycoprotein and OATPs regulate intestinal permeability of atazanavir and may contribute to its poor oral bioavailability and drug-drug interactions with other protease inhibitors and TDF.
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Registered trials
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.