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EZN-2208 + cetuximab + irinotecan

Development stage
Unknown
Lead developer
Enzon Pharmaceuticals
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

EZN-2208 + cetuximab + irinotecan is a combination regimen under investigation for the treatment of advanced solid tumors, particularly those resistant to standard therapies. EZN-2208 is a water-soluble, polyethylene glycol-conjugated form of SN38, which is the active metabolite of irinotecan and acts as a topoisomerase I inhibitor[1][2][3]. PEGylation improves solubility and pharmacokinetics, allowing prolonged exposure to SN38 in tumors compared to conventional irinotecan[6]. Cetuximab is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR), inhibiting downstream signaling involved in tumor proliferation. Irinotecan itself is also a topoisomerase I inhibitor used widely in cancer therapy. The combination aims to leverage synergistic effects by combining DNA damage induction with EGFR pathway inhibition.

Brand names
Camptosar (for irinotecan)Erbitux (for cetuximab)
Other names
PEG-SN38 (for EZN-2208)SN38 polyethylene glycol conjugate (for EZN-2208)
02

Targets

TOP1 (DNA Topoisomerase I)EGFR (Epidermal growth factor receptor)

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