ArticleFrontiers in pharmacology2022
Instability Mechanism of Osimertinib in Plasma and a Solving Strategy in the Pharmacokinetics Study.
Article in Frontiers in pharmacology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 22 citations in OpenAlex.
- Article
- Integrative Phosphoproteomic and Metabolomic Analysis of Disruption of Metabolic Homeostasis in Breast Cancer: A Pilot Study.Biochemical genetics · 2026Article
- Osimertinib's Proton-Catalyzed, Pseudoconcerted EGFR Inhibition Guides Next-Generation Inhibitor Design.Journal of chemical information and modeling · 2026Article
- Early prediction of immune checkpoint inhibitor-related pneumonitis in advanced non-small cell lung cancer based on primary tumor delta-radiomics features.Frontiers in immunology · 2026Article
- CT-guided microwave ablation combined with thoracoscopic resection for multiple ground-glass nodules: a single-session treatment strategy.Frontiers in medicine · 2026Article
- The Application and Molecular Mechanisms of Mitochondria-Targeted Antioxidants in Chemotherapy-Induced Cardiac Injury.Current issues in molecular biology · 2025Review
- A novel radiomics model combining GTVp, GTVnd, and clinical data for chemoradiotherapy response prediction in patients with advanced NSCLC.Frontiers in medicine · 2025Article
- Reversed phase HPLC analysis of mobocertinib and its impurities and studies on the structure and biological activity of a new degradation product.Frontiers in chemistry · 2025Article
- Development and application of a UHPLC-MS/MS method for the simultaneous determination of firmonertinib and its main metabolite AST-5902 in rat plasma: a study on theFrontiers in pharmacology · 2025Article
- Prognostic effect of CD74 and development of a radiomic model for predicting CD74 expression in non-small cell lung cancer.Frontiers in medicine · 2025Article
- Potential interactions between traditional Chinese medicine and osimertinib: a Case Report.Frontiers in pharmacology · 2025Article
- In vitro evidence for the potential of EGFR inhibitors to decrease the TGF-β1-induced dispersal of circulating tumour cell clusters mediated by EGFR overexpression.Scientific reports · 2024Article
- Adrenal indeterminate nodules: CT-based radiomics analysis of different machine learning models for predicting adrenal metastases in lung cancer patients.Frontiers in oncology · 2024Article
- Radiomics based onFrontiers in oncology · 2024Article
- Precision lung cancer screening from CT scans using a VGG16-based convolutional neural network.Frontiers in oncology · 2024Article
- Identification of lncRNAs associated with T cells as potential biomarkers and therapeutic targets in lung adenocarcinoma.Oncology research · 2023Article
- Development and internal validation of a nomogram for predicting survival of nonoperative EGFR-positive locally advanced elderly esophageal cancers.Frontiers in oncology · 2023Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Osimertinib is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and a star medication used to treat non-small-cell lung carcinomas (NSCLCs). It has caused broad public concern that osimertinib has relatively low stability in plasma. We explored why osimertinib and its primary metabolites AZ-5104 and AZ-7550 are unstable in rat plasma. Our results suggested that it is the main reason inducing their unstable phenomenon that the Michael addition reaction was putatively produced between the Michael acceptor of osimertinib and the cysteine in the plasma matrix. Consequently, we identified a method to stabilize osimertinib and its metabolite contents in plasma. The assay was observed to enhance the stability of osimertinib, AZ-5104, and AZ-7550 significantly. The validated method was subsequently applied to perform the pharmacokinetic study for osimertinib in rats with the newly established, elegant, and optimized ultra-performance liquid chromatography-tandem mass spectrometer (UPLC-MS/MS) strategy. The assay was assessed for accuracy, precision, matrix effects, recovery, and stability. This study can help understand the pharmacological effects of osimertinib and promote a solution for the similar problem of other Michael acceptor-contained third-generation EGFR-TKI.
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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.