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**Surufatinib + octreotide** is a combination regimen consisting of surufatinib, an oral small-molecule tyrosine kinase inhibitor (TKI), and octreotide, a synthetic somatostatin analog (SSA). Surufatinib selectively targets vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), fibroblast growth factor receptor 1 (FGFR1), and colony-stimulating factor 1 receptor (CSF-1R), thereby inhibiting tumor angiogenesis and modulating the tumor immune microenvironment by targeting tumor-associated macrophages. Octreotide acts as a somatostatin receptor agonist, primarily binding to somatostatin receptors 2, 3, and 5 (SSTR2, SSTR3, and SSTR5) to inhibit the secretion of hormones and growth factors and exert antiproliferative effects. This combination is being investigated in Phase II clinical trials for the treatment of gastroenteropancreatic neuroendocrine tumors (GEP-NETs), specifically well-differentiated G1/G2 GEP-NETs, to overcome resistance and improve progression-free survival.
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