Table 1.
The FDA-approved antibody–drug conjugates
| Name | Target | Linker | Payload | Indication(s) | Year of FDA approval |
|---|---|---|---|---|---|
| Gemtuzumab ozogamicin (Mylotarg) | CD33 | Acid-labile hydrazone-based linker | Calicheamicin derivative | AML | 2000; withdrawn in 2010; reapproved in 2017 |
| Brentuximab vedotin (Adcetris) | CD30 | Cleavable valine-citrulline linker | MMAE | HL, sALCL | 2011 |
| Ado-Trastuzumab emtansine (Kadcyla) | HER2 | Non-cleavable thioether linker | DM1 | HER2-positive breast cancer | 2013 |
| Inotuzumab ozogamicin (Besponsa) | CD22 | Acid-labile hydrazone-based linker | Calicheamicin derivative | R/R B-ALL | 2017 |
| Polatuzumab vedotin-piiq (Polivy) | CD79b | Cleavable valine- citrulline linker | MMAE | R/R DLBCL | 2019 |
| Enfortumab vedotin (Padcev) | Nectin-4 | Cleavable valine-citrulline linker | MMAE | Advanced urothelial cancer | 2019 |
| Trastuzumab deruxtecan (Enhertu) | HER2 | cleavable tetrapeptide-based linker | DXd (DX-8951 derivative) | HER2-positive breast cancer | 2019 |
| Sacituzumab govitecan (Trodelvy) | Trop-2 | Cleavable CL2A linker | SN-38 | TNBC | 2020 |
| Belantamab mafodotin (Blenrep) | BCMA | Non-cleavable maleimidocaproyl (mc) linker | MMAF | R/R multiple myeloma | 2020 |
| loncastuximab tesirine-lpyl (Zynlonta) | CD19 | Cleavable valine-alanine linker | SG3199 (PBD dimer) | R/R DLBCL | 2021 |