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Pharmacovigilance imbalance analysis of VEGFR-TKI-related taste and smell disorders.
Sci Rep
January 2025
Department of pharmacy, School of Clinical Medicine, Henan Provincial People's Hospital, People's Hospital of Zhengzhou University, Henan University, No.7 Weiwu Road, Jinshui District, Zhengzhou, 450003, Henan, China.
Taste and smell disorders (TSDs) can induce diminished interest in food, inadequate nutrient intake, and emotional irregularities, particularly among cancer patients. Previous research found that the main culprits of TSD development in cancer patients are cytotoxic drugs such as taxol, fluorouracil, cyclophosphamide, and anthracycline-based drugs. The advent of targeted drugs such as vascular endothelial growth factor receptor-tyrosine kinase inhibitors (VEGFR-TKIs) has significantly extended the survival time of cancer patients, and thus widely used in clinical practice.
View Article and Find Full Text PDFUnveiling the Anti-Angiogenic Potential of Small-Molecule (Kinase) Inhibitors for Application in Rheumatoid Arthritis.
Cells
January 2025
Department of Rheumatology & Clinical Immunology, Amsterdam UMC, Meibergdreef 9, 1105 AZ Amsterdam, The Netherlands.
Rheumatoid arthritis (RA) is a chronic autoimmune disease characterized by inflammation leading to joint damage and systemic complications. Angiogenesis promotes inflammation and contributes to RA progression. This study evaluated potential anti-angiogenic effects of several compounds including small-molecule kinase inhibitors, such as sunitinib (pan-kinase inhibitor), tofacitinib (JAK-inhibitor), NIKi (NF-κB-inducing kinase inhibitor), and the integrin-targeting peptide fluciclatide, using a scratch assay and 3D spheroid-based models of angiogenesis.
View Article and Find Full Text PDFProbing structural requirements for thiazole-based mimetics of sunitinib as potent VEGFR-2 inhibitors.
RSC Med Chem
January 2025
Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University Mansoura 35516 Egypt
Novel thiazole analogs 3a, 3b, 4, 5, 6a-g, 8a, 8b, 9a-c, 10a-d and 11 were designed and synthesized as molecular mimetics of sunitinib. antitumor activity of the obtained compounds was investigated against HepG2, HCT-116, MCF-7, HeP-2 and HeLa cancer cell lines. The obtained data showed that compounds 3b and 10c are the most potent members toward HepG2, HCT-116, MCF-7 and HeLa cells.
View Article and Find Full Text PDFMFN2-mediated decrease in mitochondria-associated endoplasmic reticulum membranes contributes to sunitinib-induced endothelial dysfunction and hypertension.
J Mol Cell Cardiol
January 2025
Department of Cardiology, Harbin Medical University Cancer Hospital, NHC Key Laboratory of Cell Transplantation, Department of Cardiology, Central Laboratory, The First Affiliated Hospital of Harbin Medical University, Institute of Metabolic Disease, Heilongjiang Academy of Medical Sciences, Heilongjiang Key Laboratory for Metabolic Disorder & Cancer Related Cardiovascular Diseases, Key Laboratories of Education Ministry for Myocardial Ischemia Mechanism and Treatment, State Key Laboratory of Frigid Zone Cardiovascular Diseases (SKLFZCD), Harbin, China. Electronic address:
Unlabelled: Treatment of cancer patients with tyrosine kinase inhibitors (TKIs) often results in hypertension, but the underlying mechanism remains unclear. This study aimed to examine the role of mitochondrial morphology and function, particularly mitochondria-associated endoplasmic reticulum membranes (MAMs), in sunitinib-induced hypertension.
Methods: Both in vitro and in vivo experiments performed to assesse reactive oxygen species (ROS), nitric oxide (NO), endothelium-dependent vasorelaxation, systemic blood pressure, and mitochondrial function in human umbilical vein endothelial cells (HUVECs) and C57BL/6 mouse aortic endothelial cells, under vehicle or sunitinib treatment condition.
Persistent Thrombocytopenia of an Unexplained Cause in a Patient With Metastatic Renal Cell Carcinoma: A Case Report.
Cureus
December 2024
Surgical Oncology, Mahamana Pandit Madan Mohan Malaviya Cancer Centre, Homi Bhabha Cancer Hospital, Tata Memorial Centre, Varanasi, IND.
Thrombocytopenia is a common complication in patients with solid tumors, particularly renal cell carcinoma (RCC), arising from mechanisms such as chemotherapy, direct tumor invasion, and paraneoplastic syndromes. Managing thrombocytopenia in advanced cancer presents significant challenges, often limiting therapeutic options and impacting patient outcomes. This case report describes a 62-year-old man with metastatic RCC complicated by persistent thrombocytopenia, unresponsive to both conventional treatments and novel therapies.
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