Table 1.
ADCs approved in the USA/EU until 2020.
| ADC | Target | Payload | Linker | Indication |
|---|---|---|---|---|
| gemtuzumab ozogamicin (Mylotarg, 1) | CD33 | Calicheamicin | Cleavable, Hydrazone | Acute myeloid leukemia |
| brentuximab vedotin (Adcetris, 2) |
CD30 | MMAE 1 | Cleavable, Peptide | Hodgkin leukemia; Systemic anaplastic large-cell lymphoma |
| trastuzumab emtansine (Kadcyla, 3) | HER2 | DM1 | Non-cleavable, Thioether |
Breast cancer |
| inotuzumab ozogamicin (Besponsa, 4) |
CD22 | Calicheamicin | Cleavable, Hydrazone | B-cell Acute lymphocytic leukemia |
| polatuzumab vedotin (Polivy, 5) |
CD79b | MMAE | Cleavable, Peptide | Diffuse large B-cell lymphoma |
| enfortumab vedotin (Padcev, 6) |
Nectin-4 | MMAE | Cleavable, Peptide | Urothelial cancer |
| trastuzumab deruxtecan (Enhertu, 7) | HER2 | deruxtecan | Cleavable, Peptide | Breast cancer |
| sacituzumab govitecan (TRODELVY, 8) | TROP-2 | SN-38 | Cleavable, Peptide | Breast cancer |
| belantamab mafodotin (BLENREP, 9) |
BCMA | MMAF | Non-cleavable, Thioether? |
Multiple myeloma |
| moxetumomab pasudotox (Lumoxiti, 10) | CD22 | PE38 | Fusion protein | Hairy cell leukemia |
| tagraxofusp (Elzonris, 11) |
IL-3 | Diphteria toxin | Fusion protein | Blastic plasmacytoid dendritic cell neoplasm |
| ibritumomab tiuxetan (ZEVALIN, 12) | CD20 | 90-yttrium | tiuxetan | Multiple hematological disorders |
1 MMAE: monomethyl auristatin E; DM1: N(2′)-deacetyl-N(2′)-(3-mercapto-1-oxopropyl)- maytansine; HER2: human epidermal growth factor 2; TROP-2: antitrophoblast cell-surface antigen 2; BCMA: B-cell maturation antigen; MMAF: monomethyl auristatin F; PE38: Pseudomonas Aeruginosa exotoxin.