The cryptophycins as potent payloads for antibody drug conjugates

Vishal A Verma; Thomas H Pillow; Laura DePalatis; Guangmin Li; Gail Lewis Phillips; Andrew G Polson; Helga E Raab; Susan Spencer; Bing Zheng

doi:10.1016/j.bmcl.2014.12.070

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. Epub 2015 Jan 2.

Authors

Vishal A Verma¹, Thomas H Pillow², Laura DePalatis², Guangmin Li², Gail Lewis Phillips², Andrew G Polson², Helga E Raab², Susan Spencer², Bing Zheng²

Affiliations

¹ Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States. Electronic address: verma.vishal@gene.com.
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.

MeSH terms

Antineoplastic Agents / therapeutic use*
Cell Line, Tumor
Depsipeptides / therapeutic use*
Humans
Immunoconjugates / therapeutic use*

Substances

Antineoplastic Agents
Depsipeptides
Immunoconjugates