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Probing 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 PDFApplication of MMP-2-responsive forming injectable hydrogel in preventing the recurrence of oral squamous cell carcinoma.
RSC Adv
January 2025
Department of Radiotherapy, Air Force Medical Center, The Fourth Military Medical University, PLA No. 30 Fucheng Road, Haidian District Beijing 100142 China
Oral squamous cell carcinoma is one of the most common types of cancer. Surgical resection is one of the most important treatments at present. However, patients often suffer from regional recurrence after surgery.
View Article and Find Full Text PDFIntroduction: Sunitinib is an oral drug approved for the treatment of metastatic renal cell carcinoma. Serious cutaneous adverse reactions to sunitinib are rare, and when they occur, discontinuation of the treatment may be needed.
Case Report: A 70-year-old male patient was diagnosed with stage IV clear cell renal carcinoma and received treatment with sunitinib.
Kinomic profiling to predict sunitinib response of patients with metastasized clear cell Renal Cell Carcinoma.
Neoplasia
December 2024
Radboud University Medical Center, 6525 GA, Nijmegen, the Netherlands.
Introduction: Treatment with Sunitinib, a potent multitargeted receptor tyrosine kinase inhibitor (TKI) has increased the progression-free survival (PFS) and overall-survival (OS) of patients with metastasized renal cell carcinoma (mRCC). With modest OS improvement and variable response and toxicity predictive and/or prognostic biomarkers are needed to personalize patient management: Prediction of individual TKI therapy response and resistance will increase successful treatment outcome while reducing unnecessary drug use and expense. The aim of this study was to investigate whether kinase activity analysis can predict sunitinib response and/or toxicity using tissue samples obtained from primary clear cell RCC (ccRCC) from a cohort of clinically annotated patients with mRCC receiving sunitinib as first-line treatment.
View Article and Find Full Text PDFPurpose: The NCI-MATCH study is a tumor-agnostic platform trial enrolling patients to targeted therapies on the basis of genomic alterations. Subprotocol V investigated sunitinib in patients with tumors harboring - mutations.
Methods: EAY131-V, is an open-label, single-arm, phase II study.
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