Etirinotecan pegol

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.[2]

Etirinotecan pegol
Clinical data
Trade namesOnzeald
Other namesNKTR-102
Routes of
administration
Intravenous infusion
ATC code
Pharmacokinetic data
Protein bindingnone
Metabolitesirinotecan and its metabolites
Elimination half-life38 days
Excretionmostly via kidneys
Identifiers
CAS Number
DrugBank
UNII
KEGG
Chemical and physical data
FormulaC153H176N20O36[C8H16O4]n (n≈113)
Molar mass20,900–24,900 g/mol[1]

It works as a topoisomerase I inhibitor.[3] Chemically, it consists of four units of irinotecan (a topoisomerase I inhibitor in use since the late 1990s[4]) 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.[1]

References

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