Zymeworks Inc.
ANTI-HER2 BIPARATOPIC ANTIBODY-DRUG CONJUGATES AND METHODS OF USE

Abstract:

Anti-HER2 biparatopic antibody-drug conjugates (ADCs) in which the drug is an auristatin analogue and is conjugated to the antibody at a low average drug-to-antibody ratio (DAR), and methods of using the ADCs in the treatment of a HER2-expressing cancer. The low average DAR (<3.9) ADCs as described herein have improved tolerability and decreased toxicity as compared to a corresponding ADC having a DAR .gtoreq.3.9 when administered at the same toxin dose.