Type of Linker

Details/Features

Enzyme Cleavable Linkers

Enzyme Activable Linkers

- Specifically cleaved by tumor-associated enzymes.

- The Glu-Val-Cit linker demonstrates outstanding activity and stability.

Sulfatase-Cleavable Linkers

- Cleaved by enzymes in the lysosome, particularly sulfatases.

- Noted stability in both human and mouse plasma, and efficient payload release.

Galactosidase Cleavable Linker

- Targeted cleavage by β-Galactosidase present in the lysosome.

- Exhibits increased potency in certain ADC designs.

Lysosomal Protease-Sensitive Linkers/

- Specifically cleaved by lysosomal proteases, such as cathepsin B.

- Val-Cit stands as a frequently utilized peptide-based linker in ADC construction.

Peptide-Based Linkers

Glucuronide Linker

- Cleaved by the β-glucuronidase enzyme.

- Its hydrophilic nature makes it suitable for hydrophobic payloads.

Chemically Cleavable Linkers

Acid Sensitive Cleavable Linker

- Undergoes cleavage in acidic milieus.

- Generally not recommended for highly cytotoxic drugs.

Glutathione-Sensitive Disulfide

- Designed to be cleaved in environments with elevated glutathione, commonly found in cancer cells.

Non-Cleavable Linkers

- Require complete degradation of the antibody to release the payload.

- Superior stability in plasma.