公开(公告)号：US20170007715A1

公开(公告)日：2017-01-12

申请号：US15202822

申请日：2016-07-06

Applicant: REGENERON PHARMACEUTICALS, INC.

Inventor： Julian ANDREEV ,  Nithya THAMBI ,  Frank DELFINO ,  Joel MARTIN ,  Gavin THURSTON ,  Katherine CYGNAR ,  Nicholas PAPADOPOULOS

IPC: A61K47/48 ,  C07K16/30 ,  C07K16/22 ,  C07K16/32 ,  C07K16/28

CPC classification number: A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6879 ,  A61K2039/507 ,  A61K2039/572 ,  A61P35/00 ,  C07K14/4702 ,  C07K16/1203 ,  C07K16/18 ,  C07K16/22 ,  C07K16/28 ,  C07K16/2833 ,  C07K16/2866 ,  C07K16/2869 ,  C07K16/2896 ,  C07K16/30 ,  C07K16/32 ,  C07K16/468 ,  C07K2317/21 ,  C07K2317/31 ,  C07K2317/35 ,  C07K2317/76 ,  C07K2317/77 ,  C07K2319/00 ,  C07K2319/30 ,  C12N9/6454

Abstract: The present invention provides multispecific antigen-binding molecules and uses thereof. The multispecific antigen-binding molecules comprise a first antigen-binding domain that specifically binds a target molecule, and a second antigen-binding domain that specifically binds an internalizing effector protein. The multispecific antigen-binding molecules of the present invention can, in some embodiments, be bispecific antibodies that are capable of binding both a target molecule and an internalizing effector protein. In certain embodiments of the invention, the simultaneous binding of the target molecule and the internalizing effector protein by the multispecific antigen-binding molecule of the present invention results in the attenuation of the activity of the target molecule to a greater extent than the binding of the target molecule alone. In other embodiments of the invention, the target molecule is a tumor associated antigen, and the simultaneous binding of the tumor associated antigen and the internalizing effector protein by the multispecific antigen-binding molecule of the present invention causes or facilitates the targeted killing of tumor cells.

Abstract translation: 本发明提供多特异性抗原结合分子及其用途。 多特异性抗原结合分子包含特异性结合靶分子的第一抗原结合结构域和特异性结合内在效应蛋白的第二抗原结合结构域。 在一些实施方案中，本发明的多特异性抗原结合分子可以是能够结合靶分子和内化效应蛋白的双特异性抗体。 在本发明的某些实施方案中，通过本发明的多特异性抗原结合分子同时结合靶分子和内化效应蛋白导致目标分子的活性比所述靶分子的结合更大程度地减弱 靶分子单独。 在本发明的其它实施方案中，靶分子是肿瘤相关抗原，并且通过本发明的多特异性抗原结合分子同时结合肿瘤相关抗原和内在效应蛋白导致或促进靶向杀伤肿瘤细胞 。