Drug intelligence / Profile preview

exemestane + pazopanib

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Exemestane + pazopanib is a combination of two pharmaceutical agents used primarily in oncology research and clinical trials. Exemestane is an oral aromatase inhibitor that irreversibly binds to and inactivates the aromatase enzyme, thereby reducing estrogen production, which is essential for the growth of hormone-sensitive breast cancer cells[8]. Pazopanib is an oral small molecule tyrosine kinase inhibitor that targets multiple receptors involved in angiogenesis, including vascular endothelial growth factor receptor 1 (VEGFR1), vascular endothelial growth factor receptor 2 (VEGFR2), vascular endothelial growth factor receptor 3 (VEGFR3), platelet-derived growth factor receptor alpha (PDGFRA), platelet-derived growth factor receptor beta (PDGFRB), c-KIT, and FGFR[1][3][6]. Pazopanib inhibits tumor blood vessel formation and tumor cell proliferation. The combination may be investigated for synergistic effects in treating certain cancers where both estrogen signaling and angiogenesis are relevant.

02

Targets

CYP19A1 (Aromatase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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