ArticleBritish journal of clinical pharmacology2010
Intracellular and plasma steady-state pharmacokinetics of raltegravir, darunavir, etravirine and ritonavir in heavily pre-treated HIV-infected patients.
Article in British journal of clinical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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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
20 citing papers in PubMed, 48 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
- Plasma and intracellular pharmacokinetics of darunavir/ritonavir once daily and raltegravir once and twice daily in HIV-infected individuals.Journal of acquired immune deficiency syndromes (1999) · 2011Trial
- Plasma and intracellular (peripheral blood mononuclear cells) pharmacokinetics of once-daily raltegravir (800 milligrams) in HIV-infected patients.Antimicrobial agents and chemotherapy · 2011Trial
- Raltegravir Plasma Exposure: A Machine Learning-Based Model for its Prediction Using Limited Sampling Strategy.The AAPS journal · 2026Article
- Quantitation of methotrexate polyglutamates in human whole blood, erythrocytes and leukocytes collected via venepuncture and volumetric absorptive micro-sampling: a green LC-MS/MS-based method.Analytical and bioanalytical chemistry · 2022Article
- Toward Consensus on Correct Interpretation of Protein Binding in Plasma and Other Biological Matrices for COVID-19 Therapeutic Development.Clinical pharmacology and therapeutics · 2021Review
- Exploration of Reduced Doses and Short-Cycle Therapy for Darunavir/Cobicistat in Patients with HIV Using Population Pharmacokinetic Modeling and Simulations.Clinical pharmacokinetics · 2021Article
- Clinical Pharmacokinetics and Pharmacodynamics of Etravirine: An Updated Review.Clinical pharmacokinetics · 2020Review
- An Expandable Mechanopharmaceutical Device (3): a Versatile Raman Spectral Cytometry Approach to Study the Drug Cargo Capacity of Individual Macrophages.Pharmaceutical research · 2018Article
- Prediction of Fetal Darunavir Exposure by Integrating Human Ex-Vivo Placental Transfer and Physiologically Based Pharmacokinetic Modeling.Clinical pharmacokinetics · 2018Article
- Physiologically Based Modelling of Darunavir/Ritonavir Pharmacokinetics During Pregnancy.Clinical pharmacokinetics · 2016Article
- Drug transporters in tissues and cells relevant to sexual transmission of HIV: Implications for drug delivery.Journal of controlled release : official journal of the Controlled Release Society · 2015Review
- Observational
- Intracellular antiviral activity of low-dose ritonavir in boosted protease inhibitor regimens.Antimicrobial agents and chemotherapy · 2014Article
- A novel ultrasensitive LC-MS/MS assay for quantification of intracellular raltegravir in human cell extracts.Journal of pharmaceutical and biomedical analysis · 2012Article
- Etravirine: a review of its use in the management of treatment-experienced patients with HIV-1 infection.Drugs · 2012Review
- Pharmacokinetic modeling of plasma and intracellular concentrations of raltegravir in healthy volunteers.Antimicrobial agents and chemotherapy · 2011Article
- Efficacy of Tat-conjugated ritonavir-loaded nanoparticles in reducing HIV-1 replication in monocyte-derived macrophages and cytocompatibility with macrophages and human neurons.AIDS research and human retroviruses · 2011Article
- Evaluation of the mean corpuscular volume of peripheral blood mononuclear cells of HIV patients by a coulter counter to determine intracellular drug concentrations.Antimicrobial agents and chemotherapy · 2011Article
- Computational screening for potential drug candidates against the SARS-CoV-2 main protease.F1000ResearchArticle
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo study the steady-state plasma and intracellular pharmacokinetics of raltegravir, etravirine, darunavir and ritonavir in heavily pre-treated patients.
methodsPatients on a salvage regimen containing raltegravir, etravirine, darunavir and ritonavir were eligible for inclusion. During a 12 h dosing interval plasma and peripheral blood mononuclear cells were collected. Drug concentrations were measured using a validated LC-MS/MS assay and pharmacokinetic analysis was performed using non-linear mixed effect modelling.
resultsIrregular absorption was observed with raltegravir and darunavir, which may be caused by enterohepatic cycling. Relative bioavailability of ritonavir was low, when compared with other ritonavir regimens. Raltegravir plasma pharmacokinetics showed wide interpatient variability, while intracellular raltegravir concentrations could not be detected (<0.001 mg l(-1) in cell lysate). The intracellular to plasma ratios for etravirine, darunavir and ritonavir were 12.9, 1.32 and 7.72, respectively, and the relative standard error of these estimates were 16.3%, 12.3% and 13.0%.
conclusionsThe observed distinct intracellular accumulation indicated that these drugs have different affinity for the cellular compartment. The relatively high intracellular accumulation of etravirine may explain its efficacy and its previously described absence of PK-PD relationships in the therapeutic concentration range, when compared with other non-nucleoside reverse transcriptase inhibitors. Lastly, the intracellular concentrations of ritonavir seem sufficient for inhibition of viral replication in the cellular compartment in PI-naive patients, but not in patients with HIV harbouring PI resistance.
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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.