Table 1.
List of currently approved antibody–drug conjugates for the treatment of solid malignancies
Target | Indication | Payload | Mechanism of action | DAR | Linker | Payload t1/2 | Cycle dose | |
---|---|---|---|---|---|---|---|---|
Trastuzumab emtansine | HER2 | Breast cancer | DM1 emtansine | Tubulin inhibitor | 3.5 | Non-cleavable | NA | 3.6 mg/kg |
Trastuzumab deruxtecan | HER2 | Breast, gastric, non-small-cell lung cancer | Exatecan derivative | Topoisomerase inhibitor | 8 | Cleavable | 5.8 days | 5.4 mg/kg |
Sacituzumab govitecan | TROP2 | Breast, urothelial cancer | SN38 | Topoisomerase inhibitor | 7.6 | Cleavable | 0.75 days | 20 mg/kg |
Enfortumab vedotin | Nectin-4 | Urothelial cancer | MMAE | Tubulin inhibitor | 4 | Cleavable | 2.4 days | 3.75 mg/kg |
Tisotumab vedotin | Tissue factor | Cervical cancer | MMAE | Tubulin inhibitor | 4 | Cleavable | NA | 2 mg/kg |
Mirvetuximab soravtansine | Folate receptor alpha | Ovarian cancer | DM4 | Tubulin inhibitor | 3.4 | Cleavable | NA | 6 mg/kg |
DAR, drug-to-antibody ratio; DM1/DM4, maytansinoids; HER2, human epidermal growth factor receptor 2; MMAE, Monomethyl auristatin E; NA, not available; t1/2, half-life; TROP2, trophoblast cell surface antigen 2.