首页> 外国专利> New human humanized antibody that specifically binds to fibroblasts activating protein alpha, useful for treating cancer or tumor, and for imaging tumors associated with activated stromal fibroblasts, e.g. lung or breast cancer

New human humanized antibody that specifically binds to fibroblasts activating protein alpha, useful for treating cancer or tumor, and for imaging tumors associated with activated stromal fibroblasts, e.g. lung or breast cancer

机译：新的人源化抗体，可特异性结合成纤维细胞活化蛋白α，可用于治疗癌症或肿瘤，以及成像与活化基质成纤维细胞相关的肿瘤，例如肺癌或乳腺癌

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Human or humanized antibody, which specifically binds to fibroblasts activating protein alpha (FAPalpha ), and which is fully human or contains not more than one murine complementarity-determining region (CDR region) of the monoclonal antibody F19 (ATCC accession number HB 8269), is new. Independent claims are also included for the following: (1) antibodies having a variable region of the heavy chain (VH) consisting of a 127 (VH13), 125 (VH46) or 134 (VH50) residue amino acid sequence, all fully defined in the specification, and the variable region of light chain (VL) comprises a 118 residue amino acid sequence (VLIII25), fully defined in the specification; (2) antibodies having a coding sequence of the variable region of VH consisting of a 381 (VH13), 375 (VH46) or 402 base pair sequence, (VH50) all fully defined in the specification, and the coding sequence of the variable region of the VLL consists of a 358 base pair sequence (VLIII25), fully defined in the specification; (3) an antibody having a variable region of VH consisting of a sequence selected from two amino acids sequences each comprising 132 amino acids (VH34 or VH18), and a variable region of VL consisting 118 amino acids (VLIII43); (4) antibodies having a coding sequence of the variable region of VH consisting of a defined sequence selected from two 396 base pair sequences (VH34 or VH18), and the variable region of the VL consists of 356 base pairs (VLIII43); (5) a nucleic acid coding for an antibody of (4); (6) a recombinant DNA vector containing the nucleic acid of (3); (7) a host containing a vector of (6); (8) a process for preparing the antibody by cultivating a host of (7) under conditions where antibody protein is expressed by the host cell, and isolating the antibody protein; (9) pharmaceutical preparations containing an antibody of (4), and one or more carrier; (10) process for detecting activated stromal fibroblasts in wound healing, inflammatory processes or tumor by contacting a probe that might possibly contain activated fibroblasts, with an antibody protein under conditions for the formation of a complex between the antibody protein and its antigen; (11) antibodies comprising or corresponding to a fully defined sequence of 255, 260, 260, 253 or 262 amino acids given in the specification, and their functional variants; and (12) antibodies encoded by a 767, 782, 782, 761 or 788 base pair sequence, fully defined in the specification. - ACTIVITY : Cytostatic. No biological data is given. - MECHANISM OF ACTION : Fibroblast activating protein-alpha modulator.

机译：人或人源化抗体，其与成纤维细胞活化蛋白α（FAPalpha）特异性结合，并且是完全人类的或含有不超过一个单克隆抗体F19的鼠类互补决定区（CDR区）（ATCC登录号HB 8269），是新的。还包括以下方面的独立权利要求：（1）具有由127（VH13），125（VH46）或134（VH50）个残基氨基酸序列组成的重链（VH）可变区的抗体，均在以下位置完全定义：说明书中，轻链可变区（VL）包含118个残基氨基酸序列（VLIII25），在说明书中有完整定义。（2）具有在说明书中完全定义的由381（VH13），375（VH46）或402碱基对序列（VH50）组成的VH可变区编码序列的抗体，以及可变区的编码序列VLL的一个由358个碱基对序列（VLIII25）组成，在说明书中有完整定义; （3）一种抗体，其具有VH可变区，该可变区由选自两个氨基酸序列的序列组成，所述两个氨基酸序列各自包含132个氨基酸（VH34或VH18），以及VL的可变区，其包含118个氨基酸（VLIII43）; （4）具有VH可变区编码序列的抗体，该编码序列由选自两个396个碱基对序列（VH34或VH18）的确定序列组成，并且VL的可变区由356个碱基对（VLIII43）组成; （5）编码（4）的抗体的核酸。（6）含有（3）的核酸的重组DNA载体。（7）含有（6）的载体的宿主; （8）通过在宿主细胞表达抗体蛋白的条件下培养（7）的宿主并分离抗体蛋白来制备抗体的方法; （9）含有（4）的抗体和一种或多种载体的药物制剂; （10）在抗体蛋白与其抗原之间形成复合物的条件下，通过使可能包含活化的成纤维细胞的探针与抗体蛋白接触，来检测伤口愈合，炎性过程或肿瘤中的活化的基质成纤维细胞的方法; （11）抗体，其包含或对应于说明书中给出的255、260、260、253或262个氨基酸的完整定义序列及其功能变体; （12）由说明书中完全定义的767、782、782、761或788个碱基对序列编码的抗体。 -活动性：细胞抑制作用。没有给出生物学数据。 -作用机理：成纤维细胞活化蛋白-α调节剂。

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公开/公告号DE10013286A1

专利类型
公开/公告日2001-09-20

原文格式PDF
申请/专利权人 BOEHRINGER INGELHEIM PHARMA KG;
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申请/专利号DE2000113286
发明设计人 SCHMIDT ALEXEJ;MOOSMAYER DIETER;PFIZENMAIER KLAUS;PARK JOHN-EDWARD;GARIN-CHESA PILAR;MERSMANN MICHAEL;
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申请日2000-03-17
分类号C07K16/00;A61K38/17;C07K14/435;A61K39/395;
国家 DE
入库时间 2022-08-22 01:09:54

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