etirinotecan pegol

Etirinotecan pegol is a long-acting, PEGylated formulation of irinotecan, developed by Nektar Therapeutics for the treatment of advanced and metastatic breast cancer, particularly in patients with brain metastases. It is designed as a polymer conjugate where four units of irinotecan are linked to a central pentaerythritol ether via carboxymethyl glycine and polyethylene glycol (PEG) chains. This structure provides an extended half-life, allowing sustained release and prolonged exposure to the active metabolite SN38 within tumors. The mechanism of action involves inhibition of DNA topoisomerase I, leading to DNA breaks that inhibit replication and trigger apoptosis in cancer cells. Despite promising clinical activity, especially in breast cancer with brain metastases, the European Medicines Agency refused marketing authorization for this drug in 2017. Development has included phase II/III trials for high-grade glioma and metastatic breast cancer resistant to standard therapies.

Brand names

Onzeald

Other names

PEG-IrinotecanPegylated irinotecan