Drug intelligence / Profile preview

LY2510924 + sunitinib

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules, Peptides
Administration
Subcutaneous, Oral
01

Overview

LY2510924 + sunitinib is an investigational combination therapy consisting of **LY2510924**, a potent, selective peptide antagonist of the chemokine receptor CXCR4, and **sunitinib**, a small molecule multitargeted tyrosine kinase inhibitor. LY2510924 inhibits the CXCR4/stromal cell-derived factor-1 (SDF-1) axis, which is implicated in tumor growth, metastasis, and chemoresistance. Sunitinib targets several receptor tyrosine kinases, including vascular endothelial growth factor receptors (VEGFRs), platelet-derived growth factor receptors (PDGFRs), KIT, and FLT3, among others, inhibiting angiogenesis and tumor proliferation. The combination was primarily studied as first-line therapy for metastatic renal cell carcinoma (RCC), with the rationale that dual inhibition may enhance antitumor activity through disruption of both tumor cell migration and angiogenesis[4][6].

Other names
SUN
02

Targets

CXCR4 (C-X-C motif chemokine receptor 4)KIT (c-KIT proto-oncogene receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)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)

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