Etirinotecan pegol - CAS 1193151-09-5
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Not Intended for Therapeutic Use. For research use only.
Etirinotecan pegol, also know as pegylated irinotecan, NKTR102, is a formulation of polyethylene glycol (PEG)-encapsulated irinotecan with antineoplastic activity. The prodrug irinotecan, a semisynthetic derivative of camptothecin, is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, 7-ethyl-10-hydroxy-camptothecin inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptosis. Pegylation provides improved drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile.
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NKTR102; NKTR 102; NKTR-102; pegylated irinotecan NKTR 102; Etirinotecan pegol
Current Developer:
Nektar Therapeutics.
1.Etirinotecan pegol (NKTR-102) versus treatment of physician's choice in women with advanced breast cancer previously treated with an anthracycline, a taxane, and capecitabine (BEACON): a randomised, open-label, multicentre, phase 3 trial.
Perez EA1, Awada A2, O'Shaughnessy J3, Rugo HS4, Twelves C5, Im SA6, Gómez-Pardo P7, Schwartzberg LS8, Diéras V9, Yardley DA10, Potter DA11, Mailliez A12, Moreno-Aspitia A13, Ahn JS14, Zhao C15, Hoch U15, Tagliaferri M15, Hannah AL16, Cortes J17. Lancet Oncol. 2015 Nov;16(15):1556-68. doi: 10.1016/S1470-2045(15)00332-0. Epub 2015 Oct 22.
BACKGROUND: New options are needed for patients with heavily pretreated breast cancer. Etirinotecan pegol is a long-acting topoisomerase-I inhibitor that prolongs exposure to, but reduces the toxicity of, SN38 (the active metabolite of irinotecan). We assessed whether etirinotecan pegol is superior to currently available treatments for patients with previously treated, locally recurrent or metastatic breast cancer.
2.Etirinotecan pegol for the treatment of breast cancer.
López-Miranda E1, Cortés J1,2. Expert Opin Pharmacother. 2016 Apr;17(5):727-34. doi: 10.1517/14656566.2016.1154537. Epub 2016 Mar 10.
INTRODUCTION: Advanced breast cancer is incurable for most patients with limited therapeutic options. As such, there is a critical need for new and novel agents that lack cross-resistance and mitigate overlapping toxicities.
3.Nonclinical pharmacokinetics and activity of etirinotecan pegol (NKTR-102), a long-acting topoisomerase 1 inhibitor, in multiple cancer models.
Hoch U1, Staschen CM, Johnson RK, Eldon MA. Cancer Chemother Pharmacol. 2014 Dec;74(6):1125-37. doi: 10.1007/s00280-014-2577-7. Epub 2014 Sep 17.
PURPOSE: The aim of the study was to demonstrate the activity of etirinotecan pegol, a polymer conjugate of irinotecan, in multiple human tumor models and to establish both the pharmacokinetic/pharmacodynamics (PK/PD) relationship and clinical relevance of the findings.
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CAS 1193151-09-5 Etirinotecan pegol

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