pH-Trigger Releasable PEGs

NOF has provided pH-trigger releasable PEG derivatives having pH-cleavable acetyl linkers. The linkers can be cleaved at mildly acidic environment, such as endosomes, lysosomes, or tumor tissues, releasing the pharmaceutical substances conjugated to the linkers. The release rate of the pharmaceutical substances can be adjusted appropriately with different substituents on the benzene ring. The highly tunable linker technology is also applicable to hetero-type PEG derivatives which are useful as linkers for Antibody-Drug Conjugates (ADCs).

Function of Releasable Linker

Serum Stability

Stability in mouse or human serum at 37°C

Tunable pH-Sensitivity

The pH-sensitivity of the acetal could be controlled by changing the substituent (X) on the benzene ring. We can also provide other derivatives with different hydrolysis rates.