Trial reportBritish journal of clinical pharmacology2013
Prediction of free imatinib concentrations based on total plasma concentrations in patients with gastrointestinal stromal tumours.
Trial report in British journal of clinical pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers, 1 of them a synthesis that pooled it.
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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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
20 citing papers in PubMed, 1 synthesis or guideline pooled it, 41 citations in OpenAlex.
- Published Population Pharmacokinetic Models of Imatinib Perform Poorly on TDM Data from Pediatric Patients.Targeted oncology · 2025Pooled it
- Integrated exposure-response analysis of efficacy and safety of lurbinectedin to support the dose regimen in small-cell lung cancer.Cancer chemotherapy and pharmacology · 2022Trial
- Elevated acute phase proteins affect pharmacokinetics in COVID-19 trials: Lessons from the CounterCOVID - imatinib study.CPT: pharmacometrics & systems pharmacology · 2021Trial
- Data-driven personalization of a physiologically based pharmacokinetic model for caffeine: A systematic assessment.CPT: pharmacometrics & systems pharmacology · 2021Trial
- Precision Medicine in Oncology: Imatinib Dosing in the Obese Cancer Population Using Virtual Clinical Trials.CPT: pharmacometrics & systems pharmacology · 2025Article
- Physiologically Based Pharmacokinetic Model of Tyrosine Kinase Inhibitors to Predict Target Site Penetration, with PET-Guided Verification.CPT: pharmacometrics & systems pharmacology · 2025Article
- Disease-Drug-Drug Interaction of Imatinib in COVID-19 ARDS: A Pooled Population Pharmacokinetic Analysis.CPT: pharmacometrics & systems pharmacology · 2025Article
- Whole Body Physiologically Based Pharmacokinetic Model to Explain A Patient With Drug-Drug Interaction Between Voriconazole and Flucloxacillin.European journal of drug metabolism and pharmacokinetics · 2024Article
- Physiologically Based Pharmacokinetic Modelling to Predict Imatinib Exposures in Cancer Patients with Renal Dysfunction: A Case Study.Pharmaceutics · 2023Article
- Determination of Tyrosine Kinase Inhibitors via Capillary Electrophoresis with Tandem Mass Spectrometry and Online Stacking Preconcentration.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Physiologically Based Pharmacokinetic Modeling Approaches for Patients With SARS-CoV-2 Infection: A Case Study With Imatinib.Journal of clinical pharmacology · 2022Article
- Population pharmacokinetic modelling of imatinib in healthy subjects receiving a single dose of 400 mg.Cancer chemotherapy and pharmacology · 2022Article
- Therapeutic Drug Monitoring and Individualized Medicine of Dasatinib: Focus on Clinical Pharmacokinetics and Pharmacodynamics.Frontiers in pharmacology · 2021Review
- Article
- Towards point of care systems for the therapeutic drug monitoring of imatinib.Analytical and bioanalytical chemistry · 2020Review
- Drug Exposure to Establish Pharmacokinetic-Response Relationships in Oncology.Clinical pharmacokinetics · 2020Review
- The Steps to Therapeutic Drug Monitoring: A Structured Approach Illustrated With Imatinib.Frontiers in pharmacology · 2020Review
- Implementation of a Physiologically Based Pharmacokinetic Modeling Approach to Guide Optimal Dosing Regimens for Imatinib and Potential Drug Interactions in Paediatrics.Frontiers in pharmacology · 2019Article
- Determination of unbound fraction of pazopanib in vitro and in cancer patients reveals albumin as the main binding site.Investigational new drugs · 2016Article
- Practical guidelines for therapeutic drug monitoring of anticancer tyrosine kinase inhibitors: focus on the pharmacokinetic targets.Clinical pharmacokinetics · 2014Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTotal imatinib concentrations are currently measured for the therapeutic drug monitoring of imatinib, whereas only free drug equilibrates with cells for pharmacological action. Due to technical and cost limitations, routine measurement of free concentrations is generally not performed. In this study, free and total imatinib concentrations were measured to establish a model allowing the confident prediction of imatinib free concentrations based on total concentrations and plasma proteins measurements.
methodsOne hundred and fifty total and free plasma concentrations of imatinib were measured in 49 patients with gastrointestinal stromal tumours. A population pharmacokinetic model was built up to characterize mean total and free concentrations with inter-patient and intrapatient variability, while taking into account α1 -acid glycoprotein (AGP) and human serum albumin (HSA) concentrations, in addition to other demographic and environmental covariates.
resultsA one compartment model with first order absorption was used to characterize total and free imatinib concentrations. Only AGP influenced imatinib total clearance. Imatinib free concentrations were best predicted using a non-linear binding model to AGP, with a dissociation constant Kd of 319 ng ml(-1) , assuming a 1:1 molar binding ratio. The addition of HSA in the equation did not improve the prediction of imatinib unbound concentrations.
conclusionAlthough free concentration monitoring is probably more appropriate than total concentrations, it requires an additional ultrafiltration step and sensitive analytical technology, not always available in clinical laboratories. The model proposed might represent a convenient approach to estimate imatinib free concentrations. However, therapeutic ranges for free imatinib concentrations remain to be established before it enters into routine practice.
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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.