Drug intelligence / Profile preview

gefitinib + sunitinib

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

Overview

Gefitinib + sunitinib is a combination of two small-molecule tyrosine kinase inhibitors used in oncology research, particularly for metastatic renal cell carcinoma (RCC). Gefitinib is an epidermal growth factor receptor (EGFR) inhibitor, while sunitinib is a multi-targeted receptor tyrosine kinase inhibitor that blocks several kinases involved in tumor growth and angiogenesis, including platelet-derived growth factor receptors (PDGFR), vascular endothelial growth factor receptors (VEGFR), KIT, FLT3, CSF-1R, and RET. The combination has been studied in clinical trials to assess safety and efficacy; results indicate comparable efficacy to single-agent sunitinib with an acceptable safety profile. Both drugs are orally administered[1][2][8].

Brand names
Sutent + Iressa
Other names
SU11248 (for sunitinib)sunitinib malate
02

Targets

PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)EGFR T790M (Epidermal growth factor receptor T790M mutant)CSF1R (Macrophage colony-stimulating factor receptor)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)

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