ArticleCancer chemotherapy and pharmacology2022
Population pharmacokinetic modelling of imatinib in healthy subjects receiving a single dose of 400 mg.
Article in Cancer chemotherapy and pharmacology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers, 1 of them a synthesis that pooled it.
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Who cites it
10 citing papers in PubMed, 1 synthesis or guideline pooled it, 11 citations in OpenAlex.
- Published Population Pharmacokinetic Models of Imatinib Perform Poorly on TDM Data from Pediatric Patients.Targeted oncology · 2025Pooled it
- Clinical pharmacokinetic characteristics and the food effect of radotinib.Investigational new drugs · 2026Trial
- Target Attainment and Clinical and Biochemical Parameters Associated with the Pharmacokinetics of 12 Tyrosine Kinase Inhibitors.Clinical pharmacokinetics · 2026Article
- Influence of genetic variants of imatinib on pharmacokinetics and recurrence-free survival in postoperative patients with gastrointestinal stromal tumor.European journal of clinical pharmacology · 2025Article
- Impact of Administration Time Errors on Clearance Estimation in Pharmacokinetic Analyses.Clinical and translational science · 2025Article
- Imatinib decreases germ cell survival and germline stem cell proliferation in rodent testis ex vivo and in vitro.Andrology · 2025Article
- Disease-Drug-Drug Interaction of Imatinib in COVID-19 ARDS: A Pooled Population Pharmacokinetic Analysis.CPT: pharmacometrics & systems pharmacology · 2025Article
- Body mass index affects imatinib exposure: Real-world evidence from TDM with adaptive dosing.Fundamental & clinical pharmacology · 2025Article
- Advanced gastrointestinal stromal tumor: reliable classification of imatinib plasma trough concentration via machine learning.BMC cancer · 2024Article
- Personalized Dose of Adjuvant Imatinib in Patients with Gastrointestinal Stromal Tumors: Results from a Population Pharmacokinetic Analysis.Drug design, development and therapy · 2023Article
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Authors and funding
9 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeImatinib is indicated for treatment of CML, GIST, etc. The population pharmacokinetics (popPK) of imatinib in patients under long-term treatment are reported in literature. Data obtained from bioequivalence trials for healthy subjects were used to evaluate the influence of demographic and pharmacogenetic factors on imatinib pharmacokinetics (PK) in a collective without concurrent drugs, organ dysfunction, inflammation etc. In addition, the differences in PK between the healthy subjects and a patient cohort was examined to identify possible disease effects.
methods26 volunteers were administered orally with single dose of 400 mg imatinib. 16-19 plasma samples per volunteer were collected from 0.5 up to 72 h post-dose. The popPK was built and post hoc estimates were compared with previously published PK parameters evaluated by non-compartmental analysis in the same cohort. The predictivity of the model for data collected from 40 patients with gastrointestinal stromal tumors at steady state was evaluated.
resultsThe popPK was best described by a two-compartment transit model with first-order elimination. No significant covariates were identified, probably due to the small cohort and the narrow range of demographic covariates; CYP3A5 phenotypes appeared to have some influence on the clearance of imatinib. Good agreement between non-compartment and popPK analyses was observed with the differences of the geometric means/ median of PK estimates below 10%. The model indicated lower clearance for patients compared to healthy volunteers (p value < 0.01).
conclusionThe two-compartment transit model adequately describes the absorption and distribution of imatinib in healthy volunteers. For patients, a lower clearance of imatinib compared to healthy volunteer was estimated by the model. The model can be applied for dose individualization based on trough concentrations assuming no significant differences in absorption between patients and healthy volunteers.
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