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Variations in serum concentrations of sunitinib and its metabolites in patients receiving long-term sunitinib treatment.
Cancer Chemother Pharmacol
December 2024
Division of Pharmacotherapeutics, Department of Clinical Pharmacy, School of Pharmacy, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo, 142-8555, Japan.
Purpose: The blood concentrations of some tyrosine kinase inhibitors are known to decrease with long-term administration. We evaluated the variability in the serum concentrations of sunitinib and its metabolites in patients receiving long-term sunitinib treatment.
Methods: This study prospectively recruited patients who received sunitinib for metastatic renal cell carcinoma at the Showa University Hospital between March 2020 and January 2022.
High-dose short-term osimertinib treatment is effective in patient-derived metastatic colorectal cancer organoids.
BJC Rep
April 2024
Department of Medical Oncology, Research Institute for Medical Innovation, Radboud University Medical Centre, Nijmegen, The Netherlands.
Background: Most tyrosine kinase inhibitors (TKIs) have failed in clinical trials for metastatic colorectal cancer (mCRC). To leverage the additional lower-affinity targets that most TKIs have, high-dose regimens that trigger efficacy are explored. Here, we studied unprecedented drug exposure-response relationships in vitro using mCRC patient-derived tumour organoids (PDTOs).
View Article and Find Full Text PDFUPLC-MS/MS analysis of axitinib and pharmacokinetic application in beagle dogs.
Heliyon
October 2024
College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, 471000, China.
Objective: To develop a method for determining the concentration of axitinib in beagle dog plasma and utilize this method to investigate the pharmacokinetics of orally administered axitinib in beagle dogs.
Methods: Plasma samples were processed using acetonitrile precipitation and analyzed by UPLC-MS/MS with sunitinib as an internal standard (IS). Chromatographic separation was achieved on a Waters Acquisition UPLC BEH C18 column (50 mm × 2.
Computer-Aided Design of VEGFR-2 Inhibitors as Anticancer Agents: A Review.
J Mol Recognit
January 2025
Department of Molecular Biology and Genetics, Istanbul AREL University, Istanbul, Turkey.
Due to its intricate molecular and structural characteristics, vascular endothelial growth factor receptor 2 (VEGFR-2) is essential for the development of new blood vessels in various pathological processes and conditions, especially in cancers. VEGFR-2 inhibitors have demonstrated significant anticancer effects by blocking many signaling pathways linked to tumor growth, metastasis, and angiogenesis. Several small compounds, including the well-tolerated sunitinib and sorafenib, have been approved as VEGFR-2 inhibitors.
View Article and Find Full Text PDFOral delivery of Sunitinib malate using carboxymethyl cellulose/poly(acrylic acid-itaconic acid)/Cloisite 30B nanocomposite hydrogel as a pH-responsive carrier.
BMC Biotechnol
September 2024
Faculty of Chemical and Petroleum Engineering, University of Tabriz, Tabriz, 5166616471, Iran.
Article Synopsis
- The study developed a hydrogel combining Cloisite 30B with carboxymethyl cellulose to enhance the delivery of the anticancer drug Sunitinib malate through free radical polymerization.
- Characterization of the material was conducted using techniques such as FTIR, XRD, TEM, and SEM-dot mapping, showing higher drug encapsulation efficiency with Cloisite 30B compared to the hydrogel alone.
- In vitro tests revealed that the drug release rate was affected by pH, with the Cloisite 30B-enhanced hydrogel exhibiting superior antibacterial properties and significant anticancer effects against MCF-7 cells.
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