发明名称 |
CONJUGATES INCLUDING AN ANTIBODY MOIETY, A POLYPEPTIDE THAT TRAVERSES THE BLOOD-BRAIN BARRIER, AND A CYTOTOXIN |
摘要 |
The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an antibody moiety), pharmaceutical compositions, kits (e.g., including a modified polypeptide and an as-yet unconjugated antibody), and methods of making and using the conjugates are also features of the invention. |
申请公布号 |
US2016106856(A1) |
申请公布日期 |
2016.04.21 |
申请号 |
US201314421213 |
申请日期 |
2013.08.14 |
申请人 |
AngioChem Inc. |
发明人 |
Castaigne Jean-Paul;Yang Gaoqiang;Che Christian;Demeule Michel |
分类号 |
A61K47/48;C07K16/30;C07K16/28;C07K16/32;A61K31/337 |
主分类号 |
A61K47/48 |
代理机构 |
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代理人 |
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主权项 |
1. A protein conjugate comprising an antibody moiety, a polypeptide, and a cytotoxic agent, wherein the polypeptide comprises the amino acid sequence Lys-Arg-Asn-Asn-Phe-Lys (SEQ ID NO:123) or a biologically active analog thereof. |
地址 |
Montreal CA |