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Etirinotecan pegol

From Wikipedia, the free encyclopedia
Pharmaceutical drug
Pharmaceutical compound
Etirinotecan pegol
Clinical data
Trade namesOnzeald
Other namesNKTR-102
Routes of
administration
Intravenous infusion
ATC code
Pharmacokinetic data
Protein bindingnone
Metabolitesirinotecan and its metabolites
Eliminationhalf-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 nameOnzeald) is adrug developed byNektar Therapeutics for the treatment of certain kinds ofbreast cancer withbrain metastases. TheEuropean Medicines Agency refused to grant it a marketing authorisation in 2017.[2]

It works as atopoisomerase I inhibitor.[3] Chemically, it consists of four units ofirinotecan (a topoisomerase I inhibitor in use since the late 1990s[4]) linked by carboxymethylglycine andpolyethylene glycol (PEG) chains to a centralpentaerythritol ether, resulting in a much longerbiological half-life (38 days) than that of irinotecan. It is formulated as a dihydrochloride and with 1.2 units oftrifluoroacetate.[1]

References

[edit]
  1. ^ab"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.hdl:2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/253469.PMID 28360015.
  4. ^"Drug Approval Package: Camptosar (Irinotecan Hydrochloride) NDA# 20-571/S-008".U.S.Food and Drug Administration (FDA). Retrieved25 May 2020.
SPs/MIs
(M phase)
Blockmicrotubule assembly
Block microtubule disassembly
DNA replication
inhibitor
DNA precursors/
antimetabolites
(S phase)
Folic acid
Purine
Pyrimidine
Deoxyribonucleotide
Topoisomerase inhibitors
(S phase)
I
II
II+Intercalation
Crosslinking of DNA
(CCNS)
Alkylating
Platinum-based
Nonclassical
Intercalation
Photosensitizers/PDT
Other
Enzyme inhibitors
Receptor antagonists
Other/ungrouped
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