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. |