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To assess the role of genetic polymorphisms in postoperative imatinib concentrations and edema in patients with gastrointestinal stromal tumor. The relationships between genetic polymorphisms, imatinib concentrations and edema were explored. Carriers of the rs683369 G-allele and rs2231142 T-allele had significantly higher imatinib concentrations. Grade ≥2 periorbital edemas were related to the carriership of two C-alleles in rs2072454 with an adjusted odds ratio of 2.85, two T-alleles in rs1867351 with an adjusted odds ratio of 3.42 and two A-alleles in rs11636419 with an adjusted odds ratio of 3.15. rs683369 and rs2231142 affect the metabolism of imatinib; rs2072454, rs1867351 and rs11636419 are related to grade ≥2 periorbital edemas.
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http://dx.doi.org/10.2217/pgs-2022-0171 | DOI Listing |
Target Oncol
September 2025
Department of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark.
Background: Population pharmacokinetic models can potentially provide suggestions for an initial dose and the magnitude of dose adjustment during therapeutic drug monitoring procedures of imatinib. Several population pharmacokinetic models for imatinib have been developed over the last two decades. However, their predictive performance is still unknown when extrapolated to different populations, especially children.
View Article and Find Full Text PDFBr J Cancer
September 2025
Department of Pharmacy, the First Affiliated Hospital of Ningbo University, Zhejiang, China.
Background: Adherence to imatinib may be even more limited in the adjuvant setting, as patients receiving adjuvant imatinib often do not experience disease symptoms after tumor removal. This real-world study aimed to gain insight into adherence to imatinib and the effect of adherence on treatment outcomes.
Methods: Postoperative GIST patients who visited the speciality clinic between January 2021 and September 2024 were included in the study.
Circulation
August 2025
Molecular Cardiology Research Institute (A.S., R.J.T., A.T., N.L.W., J.J.M., Q.L., I.Z.J.), Tufts Medical Center, Boston, MA.
Background: Imatinib, the first Abl-tyrosine kinase inhibitor (TKI), improved leukemia outcomes without cardiovascular side effects. Newer agents, including ponatinib, addressed imatinib resistance, improving cancer remission, but substantially increased arterial thrombotic events, including myocardial infarction (MI) and stroke. The mechanism behind ponatinib-induced thrombosis and the cardiovascular effect of asciminib, a newly approved Abl-TKI, remain unknown.
View Article and Find Full Text PDFHematology
December 2025
Jiangxi Province Key Laboratory of Immunology and Inflammation, Jiangxi Provincial Clinical Research Center for Laboratory Medicine, Department of Clinical Laboratory, The Second Affiliated Hospital, Jiangxi Medical College, Nanchang University, Nanchang, People's Republic of China.
Objectives: Chronic myeloid leukemia (CML), a clonal malignant disease arising from the BCR-ABL fusion gene, presents significant therapeutic challenges, particularly in chemotherapy resistance. The role of METTL14, a key m6A methyltransferase, is implicated in cancer biology, but its role in CML remains unclear.
Methods: Peripheral blood mononuclear cells (PBMCs) and CML cell lines (K562 and K562/G01) were conducted in vitro studies.
Adv Ther
September 2025
Clinical Pharmacology, Deciphera Pharmaceuticals LLC, 200 Smith Street, Waltham, MA, 02451, USA.
Introduction: Ripretinib, an oral switch-control inhibitor of KIT tyrosine kinase and platelet-derived growth factor receptor alpha kinase, is approved for adults with advanced gastrointestinal stromal tumor who received prior treatment with three or more kinase inhibitors, including imatinib. Ripretinib is metabolized into the equally active major metabolite DP-5439, a prominent component of total drug exposure in humans after oral administration. Ripretinib and DP-5439 undergo hepatic metabolism mainly via cytochrome P450 3A4.
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