发明名称 |
Prodrugs for beta-lactamase and uses thereof |
摘要 |
<p>The instant invention relates to a novel method for the delivery of antitumor drugs to tumor cells by the administration of a tumor-selective antibody- beta -lactamase conjugate that binds to tumor cells, and the additional administration of a cephalosporin prodrug that is converted at the tumor site, in the presence of the antibody- beta -lactamase, to an active cytotoxic drug. According to the preferred embodiment of this invention, a cephalosporin mustard has been constructed which when cleaved by beta -lactamase yields a cytotoxic nitrogen mustard. The methods, antibody-enzyme conjugate, prodrugs, pharmaceutical compositions, and combinations of this invention provide for enhanced selective killing of tumor cells and are thus useful in the treatment of cancers and other tumors.</p> |
申请公布号 |
EP0742015(A1) |
申请公布日期 |
1996.11.13 |
申请号 |
EP19960106146 |
申请日期 |
1991.11.05 |
申请人 |
BRISTOL-MYERS SQUIBB COMPANY |
发明人 |
KADOW, JOHN;KANEKO, TAKUSHI;SENTER, PETER D.;VRUDHULA, VIVEKANANDA M. |
分类号 |
A61K31/545;A61K31/546;A61K39/395;A61K47/48;A61P35/00;A61P43/00;C07D501/26;C07D501/30;C07D501/32;C07D501/34;C07D519/06;C07H15/252;(IPC1-7):A61K47/48 |
主分类号 |
A61K31/545 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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