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    METHODS AND COMPOSITIONS FOR SYNERGISTIC UPTAKE AND RETENTION OF SMALL MOLECULE LIGANDS
    1.
    发明公开
    METHODS AND COMPOSITIONS FOR SYNERGISTIC UPTAKE AND RETENTION OF SMALL MOLECULE LIGANDS 审中-公开

    公开(公告)号：US20240000979A1

    公开(公告)日：2024-01-04

    申请号：US18247427

    申请日：2021-09-28

    申请人： CORNELL UNIVERSITY

    发明人： Neil H. BANDER

    IPC分类号： A61K51/10

    CPC分类号： A61K51/1072

    摘要： The present application relates to methods of treating a subject for cancer. The method involves providing a first agent comprising a first targeting component coupled to a first cancer therapeutic component and providing a second agent comprising a second targeting component coupled to a second cancer therapeutic component. The first and second targeting components have different biodistributions and/or pharmacokinetics in the subject. The first and second agents are administered no more than eight hours apart from each other, to the subject to treat cancer. As a result of the administering, the amount of first and second cancer therapeutic component internalized and retained within a tumor is greater than the sum of first and second cancer therapeutic component internalized and retained in a tumor if each of the first and second agents were administered alone. Also disclosed is a combination therapeutic comprising the first and second agents blended together.

    METHODS AND REAGENTS FOR TUMOR TARGETING WITH GREATER EFFICACY AND LESS TOXICITY
    2.
    发明申请
    METHODS AND REAGENTS FOR TUMOR TARGETING WITH GREATER EFFICACY AND LESS TOXICITY 有权

    公开(公告)号：US20210154338A1

    公开(公告)日：2021-05-27

    申请号：US16610816

    申请日：2018-05-02

    申请人： Cornell University

    发明人： Neil H. BANDER

    IPC分类号： A61K51/10 ,  A61P35/00 ,  A61K51/04

    摘要： The present invention relates to a method for treating cancer. This method involves providing a first agent comprising a first targeting component coupled to a first cancer therapeutic component and providing a second agent comprising a second targeting component coupled to a second cancer therapeutic component. The first and second targeting components have different biodistributions and/or pharmacokinetics. The first and second agents are administered to a subject having cancer to treat the cancer. Also disclosed is a combination therapeutic comprising the first and second agents.

    METHODS AND REAGENTS FOR TUMOR TARGETING WITH GREATER EFFICACY AND LESS TOXICITY
    4.
    发明申请
    METHODS AND REAGENTS FOR TUMOR TARGETING WITH GREATER EFFICACY AND LESS TOXICITY 有权

    公开(公告)号：US20210196844A1

    公开(公告)日：2021-07-01

    申请号：US17198574

    申请日：2021-03-11

    申请人： Cornell University

    发明人： Neil H. BANDER

    IPC分类号： A61K51/10 ,  A61P35/00 ,  A61K51/04

    摘要： The present invention relates to a method for treating cancer. This method involves providing a first agent comprising a first targeting component coupled to a first cancer therapeutic component and providing a second agent comprising a second targeting component coupled to a second cancer therapeutic component. The first and second targeting components have different biodistributions and/or pharmacokinetics. The first and second agents are administered to a subject having cancer to treat the cancer. Also disclosed is a combination therapeutic comprising the first and second agents.

    Androgen Suppression, Prostate-Specific Membrane Antigen and the Concept of Conditionally Enhanced Vulnerability
    5.
    发明申请
    Androgen Suppression, Prostate-Specific Membrane Antigen and the Concept of Conditionally Enhanced Vulnerability 审中-公开
    雄激素抑制，前列腺特异性膜抗原和有条件增强的脆弱性的概念

    公开(公告)号：US20140099257A1

    公开(公告)日：2014-04-10

    申请号：US13803166

    申请日：2013-03-14

    申请人： CORNELL UNIVERSITY

    发明人： Neil H. BANDER

    IPC分类号： C07K16/40 ,  C12Q1/68 ,  G01N33/574

    CPC分类号： C07K16/40 ,  A61K49/0008 ,  A61K51/1072 ,  A61K2039/505 ,  C07K16/3069 ,  C12Q1/6886 ,  G01N33/57434 ,  G01N33/57492

    摘要： Anti-androgen therapies represent the cornerstone of prostate cancer (PC) treatment. Yet all PC patients ultimately fail efforts to rein in the androgen receptor (AR). This invention is based on the discovery that prostate-specific membrane antigen (PSMA), a highly PC-specific and clinically validated cell surface target, is AR-suppressed and up-regulated in PC as a result of hormonal manipulation. This up-regulation occurs in an unexpected timeframe and it occurs even in the castrate-resistant setting. As a result, hormonal therapy creates a state of conditionally enhanced vulnerability of PC to PSMA-targeted anti-cancer/cytotoxic agents that can be exploited by leveraging anti-AR therapy by the addition of PSMA-targeted agents. We demonstrate this conditionally enhanced vulnerability in a castrate-resistant animal model. The state of conditionally enhanced vulnerability may be relevant for other cancer targets and efforts to screen for them may improve other cancer therapies.

    摘要翻译： 抗雄激素疗法是前列腺癌（PC）治疗的基石。 然而，所有PC患者最终都不能努力控制雄激素受体（AR）。 本发明基于以下发现：由于激素操作，PC中的前列腺特异性膜抗原（PSMA）是高度PC特异性和临床验证的细胞表面靶，其被AR抑制和上调。 这种上调发生在意想不到的时间内，即使在阉割的环境中也会发生。 因此，荷尔蒙治疗产生有条件地增强PC对PSMA靶向抗癌/细胞毒性剂的脆弱性的状态，可以通过添加PSMA靶向药物来利用抗AR治疗来开发。 我们在阉割动物模型中证明了这种有条件地增强的脆弱性。 有条件增强脆弱性的状态可能与其他癌症靶点相关，并且筛选它们的努力可能会改善其他癌症治疗。

    METHODS AND REAGENTS FOR TUMOR TARGETING WITH GREATER EFFICACY AND LESS TOXICITY
    6.
    发明公开
    METHODS AND REAGENTS FOR TUMOR TARGETING WITH GREATER EFFICACY AND LESS TOXICITY 审中-公开

    公开(公告)号：US20240000980A1

    公开(公告)日：2024-01-04

    申请号：US18363369

    申请日：2023-08-01

    申请人： CORNELL UNIVERSITY

    发明人： Neil H. BANDER

    IPC分类号： A61K51/10 ,  A61P35/00 ,  A61K51/04

    CPC分类号： A61K51/1072 ,  A61K51/0402 ,  A61P35/00

    摘要： The present invention relates to a method for treating cancer. This method involves providing a first agent comprising a first targeting component coupled to a first cancer therapeutic component and providing a second agent comprising a second targeting component coupled to a second cancer therapeutic component. The first and second targeting components have different biodistributions and/or pharmacokinetics. The first and second agents are administered to a subject having cancer to treat the cancer. Also disclosed is a combination therapeutic comprising the first and second agents.

    METHODS AND COMPOSITIONS FOR INCREASING UPTAKE, INTERNALIZATION, AND/OR RETENTION OF SMALL MOLECULE LIGANDS
    7.
    发明公开
    METHODS AND COMPOSITIONS FOR INCREASING UPTAKE, INTERNALIZATION, AND/OR RETENTION OF SMALL MOLECULE LIGANDS 审中-公开

    公开(公告)号：US20230364271A1

    公开(公告)日：2023-11-16

    申请号：US18029596

    申请日：2021-09-28

    申请人： CORNELL UNIVERSITY

    发明人： Neil H. BANDER

    IPC分类号： A61K51/04 ,  A61K51/10

    CPC分类号： A61K51/0402 ,  A61K51/1072 ,  A61K2121/00

    摘要： The present application relates to methods of treating and imaging cancer. The methods involve providing a first agent comprising a first targeting component coupled to a cancer therapeutic component or an imaging component and providing a second agent comprising a second targeting component alone, wherein the second targeting component increases the uptake, internalization, and/or retention of the first targeting component coupled to a cancer therapeutic component or imaging component. The first and second agents are then administered to a subject having cancer to treat cancer. Also disclosed is a combination therapeutic or a combination imaging system, each comprising the first and second agents.

    PSMA as a BioMarker for Androgen Activity in Prostate Cancer
    8.
    发明申请
    PSMA as a BioMarker for Androgen Activity in Prostate Cancer 审中-公开
    PSMA作为前列腺癌雄激素活性的生物标志物

    公开(公告)号：US20130315830A1

    公开(公告)日：2013-11-28

    申请号：US13778306

    申请日：2013-02-27

    申请人： Cornell University

    发明人： Neil H. BANDER

    IPC分类号： G01N33/574 ,  A61K49/00

    CPC分类号： G01N33/57492 ,  A61K31/00 ,  A61K49/00

    摘要： The androgen receptor (AR) is the key driver of prostate differentiation and prostate cancer (PC) progression, and androgen ablation is the cornerstone of advanced PC treatment. Prostate-specific membrane antigen (PSMA) represents another target of interest in PC. Previous publications have reported inconsistent associations between androgen levels and PSMA expression. Using a panel of prototypical human PC cell lines, this relationship is clarified. PSMA is a biomarker that distinguishes AR-positive/PSMA-positive adenocarcinomas from AR-negative variants. PSMA is a cell surface barometer of androgen activity that can be readily identified by immunohistochemistry and/or in vivo imaging. Given that anti-androgen therapy is likely to remain a cornerstone of PC treatment, the associated up-regulation of PSMA, as well as its other characteristics, makes it a compelling target opportunity in PC.

    摘要翻译： 雄激素受体（AR）是前列腺分化和前列腺癌（PC）进展的关键驱动因素，雄激素消融是高级PC治疗的基石。 前列腺特异性膜抗原（PSMA）代表另一个PC感兴趣的目标。 以前的出版物报道了雄激素水平和PSMA表达之间的不一致的关联。 使用一组原型人类PC细胞系，澄清了这种关系。 PSMA是区分AR阳性/ PSMA阳性腺癌与AR阴性变体的生物标志物。 PSMA是可以通过免疫组织化学和/或体内成像容易地鉴定的雄激素活性的细胞表面晴雨表。 鉴于抗雄激素治疗可能仍然是PC治疗的基石，PSMA的相关上调以及其他特征使其成为PC中令人信服的目标机会。