Firtecan pegol - CAS 946062-05-1
Catalog number:
946062-05-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Description:
Firtecan pegol, also known as EZN-2208,Pegylated SN-38, or PEG-SN38, is  a water-soluble polyethyleneglycol-SN38 conjugate.  In vitro, the IC50 of EZN-2208 ranged from 3–24 nM, which was 30- to 45-fold lower than CPT-11 or 2.5- to 3.5-fold higher than SN38. In both an early-disease Raji model and an advanced-disease Daudi model, treatment with multiple doses of EZN-2208 resulted in 90% and 100% cures of animals, respectively (cure defined as no sign of tumors by gross observations at the termination of study). The activity of EZN-2208 was dramatically superior to that of CPT-11 in all three models. The excellent therapeutic efficacy of EZN-2208 in several B-cell NHL xenograft models merits its evaluation in the clinic for lymphoid malignancies.
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Synonyms:
EZN-2208 (Pegylated SN-38). PEG-SN38, Firtecan pegol
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Current Developer:
Enzon Pharmaceuticals.
1.Nonacog beta pegol (N9-GP) in haemophilia B: A multinational phase III safety and efficacy extension trial (paradigm™4).
Young G1, Collins PW2, Colberg T3, Chuansumrit A4, Hanabusa H5, Lentz SR6, Mahlangu J7, Mauser-Bunschoten EP8, Négrier C9, Oldenburg J10, Patiroglu T11, Santagostino E12, Tehranchi R3, Zak M3, Karim FA13. Thromb Res. 2016 Mar 2;141:69-76. doi: 10.1016/j.thromres.2016.02.030. [Epub ahead of print]
INTRODUCTION: Paradigm™4 was an international extension trial investigating the safety and efficacy of nonacog beta pegol, a recombinant glycoPEGylated factor IX (FIX) with extended half-life, in haemophilia B patients (FIX activity ≤2%; aged 13-70years) who had previously participated in phase III pivotal (paradigm™2) or surgery (paradigm™3) trials.
2.Measuring factor IX activity of nonacog beta pegol with commercially-available one-stage clotting and chromogenic assay kits: a two-center study.
Bowyer AE1, Hillarp A2, Ezban M3, Persson P4, Kitchen S1. J Thromb Haemost. 2016 Apr 23. doi: 10.1111/jth.13348. [Epub ahead of print]
BACKGROUND: Measurement of factor IX activity (FIX:C) using activated partial thromboplastin time (aPTT)-based one-stage clotting assays is associated with a large degree of inter-laboratory variation in samples containing glycoPEGylated recombinant FIX (rFIX), nonacog beta pegol (N9-GP). Validation and qualification of specific assays and conditions are necessary for the accurate assessment of FIX:C in samples containing N9-GP.
3.Epoetin beta pegol, but not recombinant erythropoietin, retains its hematopoietic effect in vivo in the presence of the sialic acid-metabolizing enzyme sialidase.
Aizawa K1, Kawasaki R2, Tashiro Y2, Hirata M2, Endo K2, Shimonaka Y2. Int J Hematol. 2016 Apr 15. [Epub ahead of print]
Erythropoiesis-stimulating agents (ESAs) are widely used for treating chronic kidney disease (CKD)-associated anemia. The biological activity of ESAs is mainly regulated by the number of sialic acid-containing carbohydrates on the erythropoietin (EPO) peptide. Sialidase, a sialic acid-metabolizing enzyme that accumulates in CKD patients, is suspected of contributing to shortening the circulation half-life of ESAs. Epoetin beta pegol (continuous erythropoietin receptor activator; C.E.R.A.), is an EPO integrated with methoxypolyethylene glycol (PEG). It has been suggested that C.E.R.A. may exert a favorable therapeutic effect, even under conditions of elevated sialidase; however, no detailed investigation of the pharmacological profile of C.E.R.A. in the presence of sialidase has been reported. In the present study, we injected C.E.R.A. or EPO pre-incubated with sialidase into rats, and assessed the hematopoietic effect by reticulocyte count.
4.Certolizumab pegol does not bind the neonatal Fc receptor (FcRn): Consequences for FcRn-mediated in vitro transcytosis and ex vivo human placental transfer.
Porter C1, Armstrong-Fisher S2, Kopotsha T3, Smith B4, Baker T5, Kevorkian L6, Nesbitt A7. J Reprod Immunol. 2016 Apr 14;116:7-12. doi: 10.1016/j.jri.2016.04.284. [Epub ahead of print]
Antibodies to tumor necrosis factor (anti-TNF) are used to treat inflammatory diseases, which often affect women of childbearing age. The active transfer of these antibodies across the placenta by binding of the Fc-region to the neonatal Fc receptor (FcRn) may result in adverse fetal or neonatal effects. In contrast to other anti-TNFs, certolizumab pegol lacks an Fc-region. The objective of this study was to determine whether the structure of certolizumab pegol limits active placental transfer. Binding affinities of certolizumab pegol, infliximab, adalimumab and etanercept to human FcRn and FcRn-mediated transcytosis were determined using in vitro assays. Human placentas were perfused ex vivo to measure transfer of certolizumab pegol and positive control anti-D IgG from the maternal to fetal circulation. FcRn binding affinity (KD) was 132nM, 225nM and 1500nM for infliximab, adalimumab and etanercept, respectively. There was no measurable certolizumab pegol binding affinity, similar to that of the negative control.
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CAS 946062-05-1 Firtecan pegol

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