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    Calicheamicin Conjugation by Antibody Deglycosylation
    2.
    发明申请
    Calicheamicin Conjugation by Antibody Deglycosylation 审中-公开
    卡利加霉素结合抗体脱糖基化

    公开(公告)号：US20070213511A1

    公开(公告)日：2007-09-13

    申请号：US10592438

    申请日：2005-03-15

    申请人： Arthur Kunz ,  Philip Hamann ,  Justin Moran ,  Eugene Vidunas

    发明人： Arthur Kunz ,  Philip Hamann ,  Justin Moran ,  Eugene Vidunas

    IPC分类号： C07K16/46

    CPC分类号： C07K16/30 ,  A61K39/395 ,  A61K47/6829 ,  A61K47/6849 ,  A61K47/6851 ,  C07K2317/24 ,  C07K2317/52 ,  C07K2317/73

    摘要： The present invention provides processed for preparing a calicheamicin conjugate comprising removing glycosylation of a protein and reacting (i) an activated calicheamicin—hydrolyzable linker derivative and (ii) the deglycosylated protein. In one embodiment, the protein is an antibody, such as an anti-CD33 antibody (e.g., hp67.6), an anti-CD22 antibody (e.g., G544), an anti-Lewis Y antibody (e.g., G193), an anti-5T4 antibody (e.g., H8) or an anti-CD20 antibody (e.g., rituximab). In another embodiment, the calicheamicin derivative is an N-acyl derivative of calicheamicin or a disulfide analog of calicheamicin, such as N-acetyl gamma calicheamicin dimethyl hydrazide (N-acetyl calicheamicin DMH) and the hydrolyzable linker is 4-(4-acetylephenoxy) butanoic acid (AcBut) or (3-Acetylphenyl) acetic acid (AcPAc). Also provided are calicheamicin conjugates produced by such processes.

    摘要翻译： 本发明提供加工用于制备加利车霉素缀合物的方法，包括除去蛋白质的糖基化并使（i）活化的加利车霉素可水解连接体衍生物和（ii）去糖基化蛋白质反应。 在一个实施方案中，蛋白质是抗体，例如抗CD33抗体（例如hp67.6），抗CD22抗体（例如G544），抗Lewis Y抗体（例如G193），抗 - -5T4抗体（例如H8）或抗CD20抗体（如利妥昔单抗）。 在另一个实施方案中，加利车霉素衍生物是加利车霉素的N-酰基衍生物或加利车霉素的二硫化物类似物，例如N-乙酰基γ-加利车霉素二甲基酰肼（N-乙酰加利车霉素DMH），可水解接头是4-（4-乙酰基苯氧基） 丁酸（AcBut）或（3-乙酰基苯基）乙酸（AcPAc）。 还提供了通过这些方法生产的加利车霉素缀合物。

    Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates
    5.
    发明授权
    Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates 失效
    单体加利车霉衍生物/载体缀合物的制备方法

    公开(公告)号：US5714586A

    公开(公告)日：1998-02-03

    申请号：US654505

    申请日：1996-05-28

    申请人： Martin P. Kunstmann ,  Irwin J. Hollander ,  Philip Hamann ,  Arthur Kunz

    发明人： Martin P. Kunstmann ,  Irwin J. Hollander ,  Philip Hamann ,  Arthur Kunz

    IPC分类号： A61K47/48 ,  C07K16/00 ,  A61K31/70 ,  A61K31/715 ,  C12P21/08

    CPC分类号： A61K47/48369 ,  A61K47/48407 ,  A61K47/48684

    摘要： A method is provided for preparing monomeric calicheamicin derivative/carrier conjugates with higher drug loading/yield and decreased aggregation. These conjugates are prepared by incubating a calicheamicin derivative and a proteinaceous carrier in a solution comprising a non-nucleophilic, protein-compatible, buffered solution, a cosolvent selected from the group consisting of propylene glycol, ethanol, DMSO, and combinations thereof, and an additive comprising at least one C.sub.6 -C.sub.18 carboxylic acid having a pH in the range from about 4.0 to 8.5 and at a temperature ranging from about 25.degree. C. to about 37.degree. C. for a period of time ranging from about 15 minutes to about 24 hours, and recovering monomeric calicheamicin derivative/carrier conjugates. Alternatively, the conjugates can be prepared by incubating the calicheamicin derivative and a proteinaceous carrier in a solution comprising a non-nucleophilic, protein-compatible, buffered solution and a cosolvent comprising t-butanol.

    摘要翻译： 提供了用于制备具有更高的药物负荷/产率和降低的聚集的单体加利车霉衍生物/载体缀合物的方法。 这些缀合物通过将加利车霉素衍生物和蛋白质载体在包含非亲核性，蛋白质相容性缓冲溶液，选自丙二醇，乙醇，DMSO及其组合的共溶剂的溶液中孵育来制备，以及 添加剂，其包含至少一种pH为约4.0-8.5，温度为约25℃至约37℃的C 6 -C 18羧酸，时间为约15分钟至约 24小时，并回收单体加利车霉衍生物/载体缀合物。 或者，可以通过将加利车霉素衍生物和蛋白质载体温育在包含非亲核，蛋白质相容的缓冲溶液和包含叔丁醇的助溶剂的溶液中来制备缀合物。