Linkers are key components of antibody-drug conjugates (ADCs) and their chemical and structural properties can be exploited in the design of these therapeutic agents.  We generated a panel of anti-HER2 ADCs that vary at the linker portion to examine the contribution of linker chemistry to ADC activity.  The ADCs were made using aldehyde-tagged anti-HER2 proteins conjugated using the hydrazinyl-iso-Pictet-Spengler (HIPS) ligation to a maytansine payload. The resulting ADCs were highly homogenous, with well-defined drug-to-antibody ratios (DARs).  The synthesis, cytotoxicity, stability and efficacy of the panel will be discussed.

Variation in ADC linker composition generated from aldehyde-tagged antibodies impacts both efficacy and PK

249th National Meeting (2015)

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