2. Academic Validation
  3. Synthesis of an immunoconjugate of camptothecin

Synthesis of an immunoconjugate of camptothecin

  • Bioorg Med Chem Lett. 2002 Jan 21;12(2):217-9. doi: 10.1016/s0960-894x(01)00707-7.
Michael A Walker 1,  Gene M Dubowchik,  Sandra J Hofstead,  Pamela A Trail,  Raymond A Firestone
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5100, 5 Research Parkway, Wallingford, CT 06492, USA. [email protected]
PMID: 11755358 DOI: 10.1016/s0960-894x(01)00707-7
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.

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