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    • 1. 发明申请
    • GASTRIN RELEASING PEPTIDE COMPOUNDS
    • GASTRIN释放肽化合物
    • WO2009143101A2
    • 2009-11-26
    • PCT/US2009/044447
    • 2009-05-19
    • BRACCO IMAGING S.P.A.LATTUADA, LucianoCAPPELLETTI, EnricoLINDER, Karen, E.NUNN, Adrian, D.LANTRY, Laura
    • LATTUADA, LucianoCAPPELLETTI, EnricoLINDER, Karen, E.NUNN, Adrian, D.LANTRY, Laura
    • A61K51/08
    • A61K51/088A61K49/0056G01N33/57492G01N2333/5758
    • Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.
    • 提供用于诊断,分期疾病,监测药物的治疗效果和成像患者的方法和组合物,包括放射性药物制剂。 提供了包含与放射性同位素复合的Ga-AMBA的组合物; 成像胃泌素释放肽受体(GRP-R)携带组织的成像方法以及疑似与异常GRP-R功能相关疾病的患者诊断或分期疾病的方法。 此外,提供监测靶向与GRP-R串扰的受体的药物的治疗效果的方法; 预先给药/共同给予含有GRP-R的非靶组织的方法也是如此。 特别地,提供了通过使用与GRP-R结合的配体来体内/体外监测受体和受体途径的活性的方法; 以及通过使用也可以通过外部手段检测的配体来测量与GRP-R显示串扰的受体或受体组及其相关途径的活性的方法。