Design of PEGylated soluble tumor necrosis factor receptor type I (PEG sTNF-RI) for chronic inflammatory diseases.


:A recombinant C-terminal truncated form of the human soluble tumor necrosis factor receptor type I (sTNF-RI) was produced in E. coli. This soluble receptor contains the first 2.6 of the 4 domains of the intact sTNF-RI molecule. A monoPEGylated form of this molecule was produced using a 30 kD methoxyPEG aldehyde with approximately 85% selectivity for the N-terminal amino group. This molecule was shown to be less immunogenic in primates than the full length (4.0 domain) molecule or other versions of sTNF-RI which were either PEGylated at different sites or with different molecular weight PEGs. The 30 kD PEG also has a longer serum half-life to the molecule than lower molecular weight PEGs. This molecule markedly blunts the inflammatory response in a number of rheumatoid arthritis animal models. In addition, phase I/II and early phase II data in humans indicate that PEG sTNF-RI is non-immunogenic and that weekly dosing with this drug can reduce the number of tender and swollen joints in rheumatoid arthritis patients. PEG sTNF-RI has comparable American College of Rheumatology (ACR) efficacy scores as other anti-TNF molecules currently used to treat rheumatoid arthritic patients.


Adv Drug Deliv Rev


Edwards CK 3rd,Martin SW,Seely J,Kinstler O,Buckel S,Bendele AM,Ellen Cosenza M,Feige U,Kohno T




Has Abstract


2003-09-26 00:00:00














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    journal_title:Advanced drug delivery reviews

    pub_type: 杂志文章,评审


    authors: Hammarlund-Udenaes M

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    abstract::Mitochondria represent both the main source and target of reactive oxygen and nitrogen species (RONS). In view of the large energy expenditure made by neurons during neurotransmission, an intact mitochondrial function is of paramount importance for the correct function of the brain. Accordingly, the search of therapeu...

    journal_title:Advanced drug delivery reviews

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    authors: Bolaños JP,Moro MA,Lizasoain I,Almeida A

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  • Mechanisms of TfR-mediated transcytosis and sorting in epithelial cells and applications toward drug delivery.

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    journal_title:Advanced drug delivery reviews

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    authors: Widera A,Norouziyan F,Shen WC

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    authors: Anitua E,Sánchez M,Orive G

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    journal_title:Advanced drug delivery reviews

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    authors: Weaver EM,Hummon AB

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    authors: Gumbleton M

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    pub_type: 杂志文章,评审


    authors: Zhang C,Xie B,Zou Y,Zhu D,Lei L,Zhao D,Nie H

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    pub_type: 杂志文章,评审


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    authors: Qi S,Craig D

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    pub_type: 杂志文章,评审


    authors: Barr J,Woodburn KW,Ng SY,Shen HR,Heller J

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    authors: Chung HJ,Park TG

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    journal_title:Advanced drug delivery reviews

    pub_type: 杂志文章,评审


    authors: Ginebra MP,Canal C,Espanol M,Pastorino D,Montufar EB

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    authors: Cole ET,Cadé D,Benameur H

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    pub_type: 杂志文章,评审


    authors: Weitschies W,Kosch O,Mönnikes H,Trahms L

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    authors: Biran R,Pond D

    更新日期:2017-03-01 00:00:00

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    authors: Fontana G,See E,Pandit A

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    pub_type: 杂志文章,评审


    authors: Rector RS,Payne RM,Ibdah JA

    更新日期:2008-10-01 00:00:00

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    journal_title:Advanced drug delivery reviews

    pub_type: 杂志文章,评审


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    pub_type: 杂志文章,评审


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    journal_title:Advanced drug delivery reviews

    pub_type: 杂志文章


    authors: Oku N

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    pub_type: 杂志文章,评审


    authors: Kojima R,Aubel D,Fussenegger M

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    journal_title:Advanced drug delivery reviews

    pub_type: 杂志文章,评审


    authors: Tonge SR,Tighe BJ

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    pub_type: 杂志文章,评审


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    journal_title:Advanced drug delivery reviews

    pub_type: 杂志文章,评审


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