Drug intelligence / Profile preview

cediranib + AZD0530

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Cediranib + AZD0530 is a combination regimen of two investigational oral small molecule inhibitors developed as a targeted therapy for advanced cancers, notably metastatic clear-cell renal cell carcinoma. Cediranib is a potent and selective inhibitor of vascular endothelial growth factor (VEGF) receptors VEGFR-1, VEGFR-2, and VEGFR-3, blocking angiogenesis and tumor blood vessel development. AZD0530 (saracatinib) is a potent dual inhibitor of Src and Abl tyrosine kinases; Src is implicated in cancer cell proliferation, survival, invasion, and in mechanisms of resistance to VEGF-targeted therapies. The combination aimed to overcome resistance and achieve synergistic anti-cancer effects. Both agents are orally administered and were developed by AstraZeneca for oncological indications. Clinical trials demonstrated an acceptable safety profile for the combination, though phase II data in metastatic renal cell carcinoma failed to show improved efficacy over cediranib alone.

Other names
cediranib + saracatinib
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)SFK (SRC family kinases)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR2 (Vascular endothelial growth factor receptor 2)

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