Etirinotecan pegol explained

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]

Notes and References

  1. Web site: Onzeald. European Medicines Agency. 2017-11-10.
  2. Twelves C, Cortés J, O'Shaughnessy J, Awada A, Perez EA, Im SA, Gómez-Pardo P, Schwartzberg LS, Diéras V, Yardley DA, Potter DA, Mailliez A, Moreno-Aspitia A, Ahn JS, Zhao C, Hoch U, Tagliaferri M, Hannah AL, Rugo HS . 6 . 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 . May 2017 . 28360015 . 10.1016/j.ejca.2017.02.011 . free .
  3. Web site: Drug Approval Package: Camptosar (Irinotecan Hydrochloride) NDA# 20-571/S-008 . U.S. Food and Drug Administration (FDA) . 25 May 2020.
  4. Web site: Onzeald: EPAR – Refusal public assessment report. European Medicines Agency. 2018-02-02.