Drug intelligence / Profile preview

tinengotinib + fulvestrant

Development stage
Unknown
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

JAK2 (Janus kinase 2)AURKB (Aurora kinase B)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)AURKA (Aurora kinase A)FGFR3 (Fibroblast growth factor receptor 3)JAK1 (Janus kinase 1)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)ESR1 (ERα)

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