ZymeLink™ Auristatin, is an auristatin-based drug-linker that employs an N-acylsulfonamide spacer to link the cytotoxic auristatin core to a protease sensitive linker and was designed to be highly stable and hydrophilic to closely resemble natural antibodies to possess favorable pharmacokinetics and drug exposure. Auristatins are clinically validated antibody-drug conjugate (ADC) payloads that elicit cell death by binding to microtubules and inhibiting their assembly.
ZymeLink™ Auristatin uses traceless cleavable dipeptide linkers with limited hydrophobicity and the option for either cysteine or lysine conjugation. Catabolism of the ADC following target engagement, internalization, and lysosomal trafficking releases the potent microtubule inhibitor ZD02044.
ZymeLink™ Auristatin ADCs are designed to closely resemble natural antibodies with favorable pharmacokinetics, stability, limited deconjugation and premature release of payload in circulation to maximize payload exposure at the site of action.