The cryptophycins as potent payloads for antibody drug conjugates

  • Bioorg Med Chem Lett. 2015 Feb 15;25(4):864-8. doi: 10.1016/j.bmcl.2014.12.070.
Vishal A Verma  1 ,  Thomas H Pillow  2 ,  Laura DePalatis  2 ,  Guangmin Li  2 ,  Gail Lewis Phillips  2 ,  Andrew G Polson  2 ,  Helga E Raab  2 ,  Susan Spencer  2 ,  Bing Zheng  2
Affiliations
  • 1. Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States. Electronic address: [email protected].
  • 2. Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.
PMID: 25613677 DOI: 10.1016/j.bmcl.2014.12.070
Abstract

The cryptophycins are a potent class of cytotoxic agents that were evaluated as antibody drug conjugate (ADC) payloads. Free cryptophycin analog 1 displayed cell activity an order of magnitude more potent than approved ADC payloads MMAE and DM1. This potency increase was also reflected in the activity of the cryptophycin ADCs, attached via a either cleavable or Non-cleavable Linker.

Keywords
Antibody drug conjugate; Cryptophycin.
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