Trial reportEuropean journal of cancer (Oxford, England : 1990)2013
A neuropharmacokinetic assessment of bafetinib, a second generation dual BCR-Abl/Lyn tyrosine kinase inhibitor, in patients with recurrent high-grade gliomas.
Trial report in European journal of cancer (Oxford, England : 1990), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers, 1 of them a synthesis that pooled it.
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.
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
18 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Therapeutic modulation of the blood-brain barrier in brain tumors: a systematic review of clinical and translational approaches.Cancer chemotherapy and pharmacology · 2026Pooled it
- An intracerebral microdialysis study to determine the neuropharmacokinetics of eribulin in patients with metastatic or primary brain tumors.Cancer chemotherapy and pharmacology · 2024Trial
- The effect of an adenosine AFluids and barriers of the CNS · 2018Trial
- The protein tyrosine phosphatase CD45 promotes PMN transepithelial migration, antimicrobial function, and colonic mucosal repair.JCI insight · 2026Article
- Evaluating "brain permeability": A critical issue for the development of therapeutic agents for primary and metastatic brain tumors.Neuro-oncology · 2026Review
- Pretreatment and analysis techniques development of TKIs in biological samples for pharmacokinetic studies and therapeutic drug monitoring.Journal of pharmaceutical analysis · 2024Review
- Glioma Metabolic Feedback In Situ: A First-In-Human Pharmacodynamic Trial of Difluoromethylornithine + AMXT-1501 Through High-Molecular Weight Microdialysis.Neurosurgery · 2023Article
- Differential vascular endothelial cell toxicity of established and novel BCR-ABL tyrosine kinase inhibitors.PloS one · 2023Article
- Tyrosine Kinase Inhibitors for Glioblastoma Multiforme: Challenges and Opportunities for Drug Delivery.Pharmaceutics · 2022Review
- The medicinal chemistry of mitochondrial dysfunction: a critical overview of efforts to modulate mitochondrial health.RSC medicinal chemistry · 2021Review
- Modular network mechanism of CCN1-associated resistance to HSV-1-derived oncolytic immunovirotherapies for glioblastomas.Scientific reports · 2021Article
- Feasibility of intracerebrally administering multiple doses of genetically modified neural stem cells to locally produce chemotherapy in glioma patients.Cancer gene therapy · 2021Article
- INNO-406 inhibits the growth of chronic myeloid leukemia and promotes its apoptosis via targeting PTEN.Human cell · 2020Article
- Neural Stem Cell-Based Anticancer Gene Therapy: A First-in-Human Study in Recurrent High-Grade Glioma Patients.Clinical cancer research : an official journal of the American Association for Cancer Research · 2017Article
- Src family kinases Fyn and Lyn are constitutively activated and mediate plasmacytoid dendritic cell responses.Nature communications · 2017Article
- Bafetinib (INNO-406) reverses multidrug resistance by inhibiting the efflux function of ABCB1 and ABCG2 transporters.Scientific reports · 2016Article
- A pilot microdialysis study in brain tumor patients to assess changes in intracerebral cytokine levels after craniotomy and in response to treatment with a targeted anti-cancer agent.Journal of neuro-oncology · 2014Article
- A scoping review of pediatric microdialysis: A missed opportunity for microdialysis in the pediatric neuro-oncology setting.Neuro-oncology advancesArticle
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
purposeThe primary objective of this study was to use intracerebral microdialysis (ICMD) to determine the neuropharmacokinetics of bafetinib, a dual BCR-Abl/Lyn tyrosine kinase inhibitor that may have activity against gliomas.
methodsA microdialysis catheter was placed into either peritumoural or enhancing brain tissue of seven patients at the time of tumour resection or biopsy. Twenty-four hours later, bafetinib was administered, 240 or 360 mg po, repeating the same dose 12 h later. Dialysate samples were continuously collected for 24h, with plasma samples obtained in parallel. One to two weeks after finishing ICMD, patients were allowed to resume taking bafetinib continuously while being observed for toxicity and tumour response.
resultsTwenty-six dialysate samples per patient were collected (n=6) and analysed for bafetinib by tandem mass spectrometry. Bafetinib concentrations in the brain were below the lower limit of detection of the assay (0.1 ng/ml) in all samples except one from a single subject that was 0.52 ng/ml. The mean plasma bafetinib maximum concentrations after dose 1 and 2 were 143±99 and 247±73 ng/ml, respectively. Only one patient remained on treatment past two cycles, and no radiographic responses were seen.
conclusionsBafetinib does not sufficiently cross intact or disrupted blood-brain barrier, and therefore, systemic administration of bafetinib is not recommended when investigating this drug as a treatment for brain tumours. ICMD can be a valuable research tool in early drug development. Lead-in ICMD studies can be performed relatively quickly, requiring only a small number of patients, and without significantly disrupting standard cancer care.
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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.