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    DOSAGES OF IMMUNOCONJUGATES OF ANTIBODIES AND SN-38 FOR IMPROVED EFFICACY AND DECREASED TOXICITY
    1.
    发明公开
    DOSAGES OF IMMUNOCONJUGATES OF ANTIBODIES AND SN-38 FOR IMPROVED EFFICACY AND DECREASED TOXICITY 审中-公开

    公开(公告)号：EP4035689A1

    公开(公告)日：2022-08-03

    申请号：EP22156351.3

    申请日：2013-07-23

    申请人： Immunomedics Inc.

    发明人： GOVINDAN, Serengulam V. ,  GOLDENBERG, David M.

    IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K39/00 ,  A61P35/00

    摘要： The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an antibody or antigen-binding antibody fragment. The antibody may bind to EGP-1 (TROP-2), CEACAM5, CEACAM6, CD74, CD19, CD20, CD22, CSAp, HLA-DR, AFP or MUC5ac and the immunoconjugate may be administered at a dosage of between 4 mg/kg and 24 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy.

    CONJUGATES WITH AN INTRACELLULARLY-CLEAVABLE LINKAGE
    2.
    发明公开
    CONJUGATES WITH AN INTRACELLULARLY-CLEAVABLE LINKAGE 审中-公开

    公开(公告)号：EP3939617A1

    公开(公告)日：2022-01-19

    申请号：EP21189065.2

    申请日：2009-12-02

    申请人： Immunomedics, Inc.

    发明人： GOVINDAN, Serengulam V. ,  MOON, Sung-Ju ,  GOLDENBERG, David M.

    IPC分类号： A61K47/68 ,  A61P35/00 ,  A61P31/18 ,  A61P37/02

    摘要： The present invention relates to a process for preparing a CL2A-SN-38 compound, comprising: (a) derivatizing an SN-38 drug with a first linker, wherein the first linker contains a reactive moiety that is capable of combining with a second linker, a PEG moiety comprising 8 monomeric subunits, a lysine amino acid spacer between the drug and the first linker, and a carbonate intracellularly-cleavable moiety, which is cleavable by intracellular peptidases or cleavable by the low pH environment of endosomal and lysosomal vesicles; (b) providing a second linker, which contains a targeting-moiety-coupling group, which is a maleimide group, and further contains a reactive group capable of reacting with the drug-first linker conjugate; and (c) reacting the second linker with the drug-first linker conjugate by a copper (+1) ion-catalyzed acetylene-azide cycloaddition reaction, to produce a compound having a structure represented by:

    ANTI-TROP-2 ANTIBODY-DRUG CONJUGATES AND USES THEREOF
    4.
    发明公开
    ANTI-TROP-2 ANTIBODY-DRUG CONJUGATES AND USES THEREOF 审中-公开
    抗逆转录酶-2抗体克隆抗体在VERWENDUNGEN DAVON

    公开(公告)号：EP3049443A1

    公开(公告)日：2016-08-03

    申请号：EP14847616.1

    申请日：2014-07-01

    申请人： Immunomedics, Inc.

    发明人： GOVINDAN, Serengulam V. ,  GOLDENBERG, David M.

    IPC分类号： C07K16/30

    CPC分类号： C07K16/30 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6857 ,  A61K47/6859 ,  A61K47/6863 ,  A61K47/6889 ,  A61K2039/505 ,  A61K2039/545 ,  C07K2317/24 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/77

    摘要： Described herein are compositions and methods of use of antibody-drug conjugates (ADCs) comprising an anti-Trop-2 antibody or antigen-binding fragment thereof, conjugated to one or more cytotoxic drugs. Preferably, the antibody is an RS7, 162-46.2 or MAB650 antibody. More preferably, the antibody is humanized. Preferably the drug is SN-38, pro-2-pyrrolinodoxorubicin, paclitaxel, calichemicin, DM1, DM3, DM4, MMAE, MMAD or MMAF. The compositions and methods are of use to treat Trop-2 expressing cancers, such as breast, ovarian, cervical, endometrial, lung, prostate, colon, stomach, esophageal, bladder, renal, pancreatic, thyroid, epithelial or head-and-neck cancer. Preferably, the cancer is one that is resistant to one or more standard cancer therapies. More preferably, the anti-Trop-2 antibody binds to Trop-2 expressed on normal cells, but administration of the anti-Trop-2 ADC to human cancer patients at a therapeutically effective dosage produces only limited toxicity.

    摘要翻译： 本文描述了与一种或多种细胞毒性药物缀合的包含抗Trop-2抗体或其抗原结合片段的抗体 - 药物偶联物（ADC）的组合物和方法。 优选地，抗体是RS7,162-46.2或MAB650抗体。 更优选地，将抗体人源化。 优选地，药物是SN-38，前-2-吡咯烷氧基多柔比星，紫杉醇，卡立西林，DM1，DM3，DM4，MMAE，MMAD或MMAF。 组合物和方法可用于治疗Trop-2表达的癌症，例如乳腺癌，卵巢癌，子宫颈癌，子宫内膜癌，肺癌，前列腺癌，结肠癌，胃癌，食道癌，膀胱癌，肾癌，胰腺癌，甲状腺癌，上皮癌或头颈癌 癌症。 优选地，癌症是对一种或多种标准癌症疗法有抗性的癌症。 更优选地，抗Trop-2抗体结合在正常细胞上表达的Trop-2，但是以治疗有效剂量向人类癌症患者施用抗Trop-2 ADC仅产生有限的毒性。

    IMPROVED METHOD FOR PREPARING CONJUGATES OF PROTEINS AND CHELATING AGENTS
    6.
    发明公开
    IMPROVED METHOD FOR PREPARING CONJUGATES OF PROTEINS AND CHELATING AGENTS 有权
    用于生产抗体偶联DOTA

    公开(公告)号：EP1689448A2

    公开(公告)日：2006-08-16

    申请号：EP04821464.7

    申请日：2004-12-01

    申请人： Immunomedics Inc.

    发明人： GRIFFITHS, Gary L. ,  GOVINDAN, Serengulam V.

    IPC分类号： A61K51/08

    CPC分类号： A61K51/1027 ,  A61K51/0482 ,  A61K51/1045

    摘要： Improved synthesis methods are provided for preparing conjugates of proteins and chelating agents. In the synthesis methods, non-stable bonds are hydrolyzed after the conjugate is synthesized, for example by treating the conjugate with a quenching agent. The synthesis method provides conjugates that are substantially free of non-stable bonds between the protein and the chelating agent, such that the chelating agent is less likely to dissociate with the conjugate after the conjugate has been stored for extended periods. The conjugate may be useful for therapeutic or diagnostic methods.