Drug intelligence / Profile preview

losartan + sunitinib

Development stage
Unknown
Lead developer
University of Colorado Denver
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy consists of the angiotensin II receptor blocker losartan and the multi-tyrosine kinase inhibitor sunitinib. Developed by the University of Colorado, Denver, the regimen is currently being evaluated in a Phase I/Ib clinical trial (NCT03900793) for the treatment of pediatric and adult patients with relapsed or refractory osteosarcoma. Losartan, traditionally used as an antihypertensive, is repurposed in this context to block the CCL2-CCR2 signaling pathway, which inhibits monocyte recruitment and tumor metastasis. Sunitinib provides complementary antiangiogenic and antitumor effects by targeting vascular endothelial growth factor receptors (VEGFR) and other receptor tyrosine kinases. This dual-mechanism approach aims to disrupt the tumor microenvironment and prevent cancer spread. The therapy's transition to human trials followed successful results in canine osteosarcoma studies conducted at Colorado State University.

Other names
losartan and sunitinib
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)AGTR1 (Angiotensin II Type-1 receptor)ACE (Angiotensin Converting Enzyme)MET (Mesenchymal-epithelial transition factor receptor)FGFR1 (Fibroblast growth factor receptor 1)PDGFRB (Platelet-derived growth factor receptor beta)CSF1R (Macrophage colony-stimulating factor receptor)ABL2 (ABL proto-oncogene 2, non-receptor tyrosine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRA (Platelet-derived growth factor receptor alpha)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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