公开(公告)号：WO2013046163A1

公开(公告)日：2013-04-04

申请号：PCT/IB2012/055183

申请日：2012-09-28

申请人： INVECTORS S.R.L.

发明人： ACCARDO, Antonella ,  TESAURO, Diego ,  MORELLI, Giancarlo ,  PEDONE, Carlo ,  DE ROSA, Giuseppe ,  SALZANO, Giuseppina

IPC分类号： A61K47/48 ,  A61K51/12 ,  A61K9/127

CPC分类号： A61K9/127 ,  A61K9/1273 ,  A61K31/704 ,  A61K47/6911 ,  A61K51/1234

摘要： Delivery systems based on liposomes functionalized with peptides and chelating agents, for therapy and imaging by selective targeting of tumour cells expressing the receptors GRP, BBl, BB2, BB3 e BB4 and any other receptor which recognizes the bombesin peptide or analogues thereof are described. In particular, the liposomes contain within them cytotoxic drugs, such as for example doxorubicin, for target-selective antitumour therapy, and, through the presence of the chelating agent, can contain radioactive or paramagnetic ions for the real time visualization of the tumour cells. The liposomes described in this invention thus act as a selective delivery system for drugs and/or contrast agents onto tumour cells expressing the receptors for the class of known peptides such as bombesin (endogenous sequence, analogous or peptidomimetic peptides, agonists or non agonists).

摘要翻译： 描述了基于用肽和螯合剂官能化的脂质体的递送系统，用于通过选择性靶向表达受体GRP，BB1，BB2，BB3e BB4的肿瘤细胞和识别bombesin肽或其类似物的任何其他受体来进行治疗和成像。 特别地，脂质体包含细胞毒性药物，例如多柔比星，用于靶选择性抗肿瘤治疗，并且通过螯合剂的存在，可以含有放射性或顺磁性离子，用于肿瘤细胞的实时可视化。 因此，本发明中描述的脂质体用作药物和/或造影剂在表达用于已知肽类的受体（例如铃蟾肽（内源序列，类似物或肽模拟肽，激动剂或非激动剂））的选择性递送系统。