Etirinotecan pegol

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Etirinotecan pegol
Etirinotecan pegol.svg
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]

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]

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

  1. ^ a b "Onzeald: EPAR – Refusal public assessment report" (PDF). European Medicines Agency. 2018-02-02.
  2. ^ "Onzeald". European Medicines Agency. 2017-11-10.
  3. ^ Twelves C, Cortés J, O'Shaughnessy J, Awada A, Perez EA, Im SA, et al. (May 2017). "Health-related quality of life in patients with locally recurrent or metastatic breast cancer treated with etirinotecan pegol versus treatment of physician's choice: Results from the randomised phase III BEACON trial". European Journal of Cancer. 76: 205–215. doi:10.1016/j.ejca.2017.02.011. PMID 28360015.
  4. ^ "Drug Approval Package: Camptosar (Irinotecan Hydrochloride) NDA# 20-571/S-008". U.S. Food and Drug Administration (FDA). Retrieved 25 May 2020.