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Updated: Aug 23, 2026

Analyzing Tumor and Tissue Distribution of Target Antigen Specific Therapeutic Antibody
Published on: May 16, 2020
Monoclonal antibody mediated intracellular targeting of tallysomycin S(10b)
Michael A Walker1, H Dalton King, Richard A Dalterio
1Bristol-Myers Squibb Pharmaceutical Research Institute, Medicinal Chemistry, PO Box 5100, 5 Research Parkway, Wallingford, CT 06492, USA. michael.a.walker@bms.com
Abstract:
The potency of tallysomycin S(10b) (TLM S(10b)) an analogue bleomycin was enhanced by up to 875-fold when it was conjugated to the internalizing antibody BR96. Attachment to the antibody is achieved via a Cathepsin B cleavable linker. The enhancement in potency is believed to be a result of cellular uptake of the conjugate upon antigen binding followed by rapid release of the drug inside the lysosome. This method provides a novel approach for increasing the potency and therapeutic index of nominally moderately-active cytotoxic agents.
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