AEE788 + everolimus

AEE788 + everolimus is an experimental combination therapy evaluated for the treatment of recurrent or relapsed glioblastoma multiforme. **AEE788** is an orally active small molecule tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR); **everolimus** is an mTOR (mammalian target of rapamycin) inhibitor. The rationale for combining both agents is to simultaneously inhibit upstream receptor tyrosine kinase signaling and downstream mTOR signaling pathways, thus achieving more potent blockade of tumor growth and angiogenesis. The combination was investigated in Phase I/II clinical trials to determine its safety, pharmacokinetics, and anti-tumor activity and showed synergistic effects in preclinical glioma models. However, clinical development was terminated before maximum tolerated dose was established due to safety findings in monotherapy studies.

Brand names

everolimus (sold under brand names such as Afinitor)none for AEE788 as it was never marketed

Other names

CAEE788A2106CAEE-788A2106CAEE 788A2106UCLA-0409004-01UCLA0409004-01UCLA 0409004-01CDR0000422335CDR-0000422335CDR 0000422335