Drug intelligence / Profile preview

pazopanib + metformin

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

Overview

**Pazopanib + metformin** is an investigational combination therapy pairing pazopanib, a multi-targeted tyrosine kinase inhibitor that blocks vascular endothelial growth factor receptors (VEGFR1-3), platelet-derived growth factor receptors (PDGFRα/β), and c-Kit to inhibit angiogenesis and tumor growth, with metformin, a biguanide that activates AMP-activated protein kinase (AMPK) to suppress gluconeogenesis, enhance insulin sensitivity, and exert antitumor effects via mTOR inhibition and metabolic modulation. Primarily explored in preclinical and early clinical settings for advanced cancers including renal cell carcinoma (RCC), lung cancer, and breast cancer, the combination aims to enhance antitumor synergy through complementary antiangiogenic, antiproliferative, and metabolic mechanisms, though specific clinical trials for this exact pairing remain limited and it is not an approved regimen.

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)AMPK (Adenosine monophosphate–activated protein kinase)GSEC (Gamma-Secretase Complex)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)ND1 (Mitochondrial electron transport chain complex I)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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