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tinengotinib + fulvestrant
- Development stage
- Phase 2
- Lead developer
- TransThera Biosciences
- Modality
- Small Molecules
- Administration
- Oral, Intramuscular
01
Overview
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.
- Other names
- TT-00420 + fulvestrant
02
Targets
AURKA (Aurora kinase A)AURKB (Aurora kinase B)CSF1R (Macrophage colony-stimulating factor receptor)ESR1 (ERα)FGFR1 (Fibroblast growth factor receptor 1)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)JAK1 (Janus kinase 1)JAK2 (Janus kinase 2)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR4 (Vascular endothelial growth factor Receptor-3)
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