Tradename: | Onzeald |
Routes Of Administration: | Intravenous infusion |
Atc Prefix: | L01 |
Atc Suffix: | CE03 |
Protein Bound: | none |
Metabolites: | irinotecan and its metabolites |
Elimination Half-Life: | 38 days |
Excretion: | mostly via kidneys |
Cas Number: | 848779-32-8 |
Drugbank: | DB14951 |
Kegg: | D10367 |
Unii: | LJ16641SFT |
Synonyms: | NKTR-102 |
Chemical Formula: | C153H176N20O36[C<sub>8</sub>H<sub>16</sub>O<sub>4</sub>]n (n≈113) |
Molecular Weight: | 20,900–24,900 g/mol |
Etirinotecan pegol (trade name Onzeald) is a drug developed by Nektar Therapeutics for the treatment of certain kinds of breast cancer with brain metastases. The European Medicines Agency refused to grant it a marketing authorisation in 2017.[1]
It works as a topoisomerase I inhibitor.[2] Chemically, it consists of four units of irinotecan (a topoisomerase I inhibitor in use since the late 1990s[3]) linked by carboxymethyl glycine and polyethylene glycol (PEG) chains to a central pentaerythritol ether, resulting in a much longer biological half-life (38 days) than that of irinotecan. It is formulated as a dihydrochloride and with 1.2 units of trifluoroacetate.[4]