LONG-CIRCULATING THERANOSTIC AGENTS FOR DIAGNOSING AND IMAGING METASTATIC TUMORS

    公开(公告)号:US20200206358A1

    公开(公告)日:2020-07-02

    申请号:US16719615

    申请日:2019-12-18

    发明人: Yesen Li Zhen Cheng

    摘要: Theranostic agents useful for imaging and treating metastatic cancer are provided. The theranostic agents comprise a TMTP1 peptide conjugated to an albumin binding moiety to prolong circulation lifetime and a chelating agent to allow complexation of a diagnostic metal ion with the theranostic agent. The theranostic agent can be conjugated, for example, to a positron-emitting metal radionuclide suitable for PET imaging such as 64Cu, 68Ga, 44Sc, 86Y, 89Zr, or 82Rb; or a gamma-emitting metal radionuclide suitable for single photon emission computed tomography (SPECT) imaging such as 67Ga, 99mTc, 111In, or 177Lu. Alternatively, theranostic agents can be conjugated with a paramagnetic metal ion suitable for use in magnetic resonance imaging (MRI) such as manganese (e.g., Mn2+), iron (e.g., Fe3+, Fe2+) or gadolinium (e.g., Gd3+). Such theranostic agents show selective uptake by metastatic cancer cells and are useful for PET, SPECT, or MRI imaging of metastatic cells in vitro and in vivo.

    Probes, Methods of Making Probes, and Methods of Use
    3.
    发明申请
    Probes, Methods of Making Probes, and Methods of Use 审中-公开
    探针,探针方法和使用方法

    公开(公告)号:US20140356283A1

    公开(公告)日:2014-12-04

    申请号:US14288441

    申请日:2014-05-28

    CPC分类号: A61K51/088 Y10T428/2982

    摘要: Embodiments of the present disclosure provide for water soluble polyethylene glycol (PEG)-polymeric melanin (PEG-melanin) nanoparticles, methods of using the PEG-melanin nanoparticle, methods of making the PEG-melanin nanoparticle, methods of imaging a diseases or condition (e.g., pre-cancerous tissue, cancer, or a tumor), and the like. Embodiments of the present disclosure can be used in multimodal imaging (e.g., photoacoustic, nuclear, magnetic, fluorescent, and the like).

    摘要翻译: 本发明的实施方案提供了水溶性聚乙二醇(PEG) - 聚合黑色素(PEG-黑色素)纳米颗粒,使用PEG-黑色素纳米颗粒的方法,制备PEG-黑色素纳米颗粒的方法,成像疾病或病症的方法 例如癌前组织,癌症或肿瘤)等。 本公开的实施例可以用于多模式成像(例如光声,核,磁,荧光等)。

    RADIOLABELED BBN ANALOGS FOR PET IMAGING OF GASTRIN-RELEASING PEPTIDE RECEPTORS
    5.
    发明申请
    RADIOLABELED BBN ANALOGS FOR PET IMAGING OF GASTRIN-RELEASING PEPTIDE RECEPTORS 审中-公开
    胃肠吸收肽受体PET成像的放射性BBN模拟

    公开(公告)号:US20130323171A1

    公开(公告)日:2013-12-05

    申请号:US13910318

    申请日:2013-06-05

    IPC分类号: C07K7/08 G01N33/50 A61K51/08

    摘要: Radiolabeled bombesin (BBN) analogs that bind to the gastrin-releasing peptide receptor (GRPR) represent a topic of active investigation for the development of molecular probes for positron emission tomography (PET) or single-photon emission computed tomography (SPECT) of prostate cancer (PCa). RM1 and AMBA have been identified as the two most promising BBN peptides for GRPR-targeted cancer imaging and therapy. In this study, to develop a clinically translatable BBN-based PET probe, we synthesized and evaluated 18F—AlF- and 64Cu-radiolabeled RM1 and AMBA analogs for their potential application in PET imaging of PCa.

    摘要翻译: 结合胃泌素释放肽受体(GRPR)的放射性标记的bombesin(BBN)类似物代表了正面发射断层扫描(PET)或单光子发射计算机断层扫描(SPECT)前列腺癌分子探针的研究的主题。 (PCa)。 已经将RM1和AMBA鉴定为用于GRPR靶向癌症成像和治疗的两种最有希望的BBN肽。 在本研究中,为了开发临床可翻译的基于BBN的PET探针,我们合成并评估了18F-AlF和64Cu放射性标记的RM1和AMBA类似物在PCa PET成像中的潜在应用。

    Cystine knot peptides that bind alpha-V-beta-6 integrin
    8.
    发明授权
    Cystine knot peptides that bind alpha-V-beta-6 integrin 有权
    结合α-V-β-6整联蛋白的胱氨酸结结肽

    公开(公告)号:US09206237B2

    公开(公告)日:2015-12-08

    申请号:US14283830

    申请日:2014-05-21

    摘要: Disclosed are peptides comprising a molecular scaffold portion and a loop portion that binds to integrin αvβ6. This integrin is expressed on pancreatic tumors, making the peptides useful as imaging agents, among other uses. The peptides showed single-digit nanomolar dissociation constants similar to antibodies used clinically for imaging and therapy. The peptides rapidly accumulated in αvβ6-positive tumors, which led to excellent tumor-to-normal contrast. The peptides are specific for the targeted integrin αvβ6 receptors expressed on orthotopic pancreatic tumors and various xenografts used. Additionally, pharmacokinetic-stabilization strategies endowed knots with rapid renal clearance, which significantly reduced off-target dosing.

    摘要翻译: 公开了包含分子支架部分和结合整联蛋白αv&bgr的环部分的肽6。 这种整合素在胰腺肿瘤中表达,使得肽可用作成像剂,以及其他用途。 这些肽显示出与临床上用于成像和治疗的抗体相似的单位纳摩尔解离常数。 肽在6个阳性的肿瘤中迅速积累,导致肿瘤与正常的对比。 这些肽对于在原位胰腺肿瘤和各种​​异种移植物上表达的靶向整合素αv和bgr 6受体是特异性的。 此外,药代动力学稳定化策略赋予了快速肾清除的结,这显着降低了靶外给药。