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Tinengotinib + fulvestrant is a combination therapy being developed by TransThera Sciences for the treatment of hormone receptor-positive (HR+) and human epidermal growth factor receptor 2 (HER2)-negative or low-expressing recurrent or metastatic breast cancer. Tinengotinib (TT-00420) is an oral, small-molecule, spectrum-selective kinase inhibitor that targets Aurora kinases (A and B), vascular endothelial growth factor receptors (VEGFR 1-3), fibroblast growth factor receptors (FGFR 1-3), Janus kinases (JAK 1/2), and colony-stimulating factor 1 receptor (CSF1R). Fulvestrant is an injectable selective estrogen receptor degrader (SERD). This combination aims to overcome resistance to prior endocrine therapies and CDK4/6 inhibitors by simultaneously targeting tumor cell mitosis, angiogenesis, and the tumor microenvironment. The combination is currently being evaluated in Phase II clinical trials, particularly for patients who have failed prior treatments including CDK4/6 inhibitors.
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