Cleavable pendant type PEG linker

NOF has developed cleavable pendant type PEG linker. The pendant type PEG linkers have dipeptide and selfimmolative moiety that are cleaved by lysosomal enzyme and can release native drugs.

We prepared ADCs with the cleavable pendant type PEG linker. We evaluated the hydrophobicity of the ADC by hydrophobic interaction chromatography (HIC) and performed in vivo pharmacokinetic study, in vitro cytotoxic study, in vivo mice single dose tolerability study and anti-tumor activity study. The results demonstrated that the cleavable pendant type PEG linker using PEG12 improved hydrophilicity, pharmacokinetics and anti-tumor activity of the ADC more effectively by masking hydrophobicity of drugs.

In vitro Cytotoxicity of ADCs

In vivo Single dose mice tolerability of ADCs

In vivo Anti-tumor activity of ADCs