Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0677930 (primary tumor)
 20,210 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Sunitinib (SU-11248, Sutent) inhibits at least eight receptor protein-tyrosine kinases including vascular endothelial growth factor receptors 1-3 (VEGFR1-VEGFR3), platelet-derived growth factor receptors (PDGFRalpha and PDGFRbeta), stem cell factor receptor (Kit), Flt-3, and colony-stimulating factor-1 receptor (CSF-1R). VEGFR1 and VEGFR2 play key roles in vasculogenesis and angiogenesis. PDGFRbeta, which is found in pericytes that surround capillary endothelial cells, plays a pivotal role in stabilizing the vascular endothelium. Sunitinib inhibits angiogenesis by diminishing signaling through VEGFR1, VEGFR2, and PDGFRbeta. Renal cell cancers that have metastasized, or spread from the primary tumor, exhibit extensive vascularity, and sunitinib is approved for the treatment of these neoplasms. Activating Kit mutations occur in about 85% of gastrointestinal stromal tumors and activating PDGFRalpha mutations occur in about 5% of these tumors. Sunitinib is approved for the treatment of those tumors that are resistant to imatinib (STI-571, Gleevec), another Kit and PDGFRalpha protein-tyrosine kinase inhibitor. Both sunitinib and imatinib bind reversibly to the ATP binding site of their target kinases and thereby inhibit their catalytic activity.
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PMID:Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. 1736 63

A 39 years old male patient with a history of an unresectable thymoma and synchronous liver metastases was referred tor our position. The patient had been originally treated with systemic chemotherapy followed by imatinib (Glivec) and sunitinib (Sutent). Since the therapeutic response was unsatisfactory, a gallium-68 ((68)Ga)-Dotatoc-positron emission tomography (PET) was performed and demonstrated an enhanced SSTR 2 expression in the primary tumor but not in the liver metastases. Three cycles of yttrium-90 ((90)Y)-Dotatoc were then administered. Outcome after treatment was monitored by (18)F-FDG-PET and CT and showed a response only of the primary tumor. Selective internal radiation treatment (SIRT) with (90)Y microspheres was then applied for the liver metastases. (18)F-FDG uptake showed that metabolism in the liver metastases decreased after SIRT. MRI of the liver demonstrated a decrease in vascularization and a modest decrease in tumor volume. Therefore, surgical resection of the primary thymoma was initiated.
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PMID:Treatment monitoring with 18F-FDG PET in metastatic thymoma after 90Y-Dotatoc and selective internal radiation treatment (SIRT). 1993 42

The development of targeted agents has expanded the anticancer arsenal available to oncologists and revolutionized the field of cancer treatment. In patients with advanced renal cell carcinoma (RCC), small molecule targeted therapies have improved clinical outcomes compared with cytokine-based treatments. Sunitinib malate is one such drug that has demonstrated clinical efficacy in patients with metastatic renal cell carcinoma (mRCC). This oral, multi-targeted tyrosine kinase inhibitor is approved for use in multiple countries for the treatment of advanced RCC and gastrointestinal stromal tumor patients who have progressed on imatinib therapy. In patients with advanced RCC, sunitinib significantly improves clinical outcomes with a favorable safety profile compared with conventional treatment with interferon-a. The clinically proven treatment and safety outcomes have led investigators to evaluate the merits of sunitinib therapy in the adjuvant and neoadjuvant setting in patients with mRCC. In the neoadjuvant setting, preliminary data suggest that sunitinib can effectively reduce the primary tumor and facilitate surgical resection in patients with locally advanced and mRCC. Post-operative complications were observed in some patients, but the overall safety profile and efficacy suggests that mRCC patients with surgically inoperable tumors may benefit from neoadjuvant sunitinib therapy. Ongoing clinical trials should provide insight into the value of sunitinib as adjuvant therapy.
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PMID:Current evidence and the evolving role of sunitinib in the management of renal cell carcinoma. 2714 54