Drug intelligence / Profile preview

aee788

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

AEE788 is an orally bioavailable small molecule multikinase inhibitor developed as an anticancer agent. It potently inhibits the tyrosine kinase activity of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2/ErbB2), and vascular endothelial growth factor receptor 2 (VEGFR2/KDR). By blocking phosphorylation of these receptors, AEE788 inhibits cellular proliferation and angiogenesis, induces apoptosis in tumor cells and tumor-associated endothelial cells, and suppresses tumor growth. The drug was primarily investigated for the treatment of various cancers including glioblastoma multiforme and solid tumors. Clinical development was discontinued due to unacceptable toxicity and limited efficacy[1][3][4][6].

Other names
6-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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