NOF has developed cleavable pendant type PEG linker. This linker has Lysosomal enzyme cleavage site constituted of dipeptide unit and self-immolative moiety unit, which enables intracellular drug release in native form.
Proof of Concept
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.
