Drug intelligence / Profile preview

dovitinib + aromatase inhibitor

Development stage
Unknown
Lead developer
Allarity Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Dovitinib + aromatase inhibitor is a combination therapy investigated for the treatment of hormone receptor-positive (HR+), HER2-negative metastatic breast cancer. This regimen combines dovitinib (TKI258), an investigational multi-targeted tyrosine kinase inhibitor, with a standard-of-care aromatase inhibitor (AI) such as anastrozole, letrozole, or exemestane. Dovitinib inhibits several key signaling pathways, including the fibroblast growth factor receptor (FGFR), vascular endothelial growth factor receptor (VEGFR), and platelet-derived growth factor receptor (PDGFR), which are thought to contribute to the development of resistance to endocrine therapies. Aromatase inhibitors function by blocking the enzyme aromatase, which is responsible for the peripheral conversion of androgens into estrogens in postmenopausal women. By combining these agents, researchers at Georgetown University aimed to overcome or delay the onset of endocrine resistance in patients who had previously progressed on AI therapy.

Other names
dovitinib + AITKI258 + aromatase inhibitor
02

Targets

CYP19A1 (Aromatase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)FGFR3 (Fibroblast growth factor receptor 3)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)

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