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Bioorg Med Chem Lett. 2002 Jan 21;12(2):217-9.

Synthesis of an immunoconjugate of camptothecin.

Author information

1
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5100, 5 Research Parkway, Wallingford, CT 06492, USA. michael.a.walker@bms.com

Abstract

The first immunoconjugate of camptothecin has been synthesized wherein the drug is attached to the tumor-recognizing antibody BR96 via a Cathepsin B cleavable linker. Endocytosis of the immunoconjugate upon binding to the tumor cell followed by enzymatic cleavage of the linker inside the endosome ensures tumor-specific release of the drug. In this way, it is hoped that the dose-limiting side effects associated with camptothecin can be eliminated while the antitumor activity is preserved.

PMID:
11755358
DOI:
10.1016/s0960-894x(01)00707-7
[Indexed for MEDLINE]

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