Drug intelligence / Profile preview

sunitinib + erlotinib

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

Overview

Sunitinib + erlotinib is a combination of two oral small-molecule tyrosine kinase inhibitors investigated primarily for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC), especially in patients who have progressed after platinum-based chemotherapy. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor that blocks several kinases involved in tumor growth and angiogenesis, including all platelet-derived growth factor receptors (PDGFR), vascular endothelial growth factor receptors (VEGFR), KIT, FLT3, CSF1R, and RET. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor that interferes with EGFR-mediated signaling pathways critical for cancer cell proliferation and survival. The combination has been evaluated in phase I–III clinical trials to determine safety, tolerability, pharmacokinetics, and antitumor activity. While the regimen was generally tolerable at specific doses (sunitinib 37.5 mg daily plus erlotinib 150 mg daily), it was associated with increased rates of certain toxicities compared to either agent alone[1][2][5]. The combination may enhance antitumor activity but also increases risks such as gastrointestinal perforation[3].

Brand names
TarcevaSutent
Other names
sunitinib malate + erlotinib hydrochloride
02

Targets

PDGFRB (Platelet-derived growth factor receptor beta)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)CSF1R (Macrophage colony-stimulating factor receptor)EGFR T790M (Epidermal growth factor receptor T790M mutant)RET (Rearranged during transfection receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)CYP1A1 (Cytochrome P450 1A1)

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