TABLE 1

List of approved ADCs with linker and payloads used

NonproprietaryYear of Approval (FDA or EMA)AntibodyConjugation and Linker ChemistryPayloadReference
Gemtuzumab ozagamicin2000, 2017mAbHydrazoneCleavable
(pH)
Calicheamycin(Ali et al., 2019)
Brentuximab vedotin2011mAbValine-CitrullineCleavable (enzymatically)MMAE(Gravanis et al., 2016)
Trastuzumab emantansine2013mAbsuccinimidyl 4-(N-maleimidomethyl) cyclohexane-1-carboxylateNoncleavablethiol-containing maytansinoid toxin(Chen et al., 2016)
Inotuzumab ozagamicin2017mAbHydrazoneCleavable
(pH)
Calicheamycin(Lamb, 2017)
Moxetumomab pasudotox2018mAb/fusion proteinrecombinant fusion, no linkerCleavable38 kDa fragment of Pseudomonas exotoxin A(Dhillon, 2018)
Polatuzumab vedotin-piiq2019mAbValine-CitrullineCleavable
(enzymatically)
MMAE(Deeks, 2019)
Enfortumab vedotin2019mAbValine-CitrullineCleavable
(enzymatically)
MMAE(Maas et al., 2021)
Trastuzumab deruxtecan2019mAbTetrapeptideCleavable
(enzymatically)
Topoisomerase I inhibitor conjugate deruxtecan(Narayan et al., 2021)
Sacituzumab govitecan2020mAbCarbonateCleavable
(pH)
SN38(Wahby et al., 2021)
Belantamab mafodotin2020mAbMaleimidocaproyl (mc) linkerNon cleavableMonomethyl auristatin F(Markham, 2020)
Loncastuximab tesirine2021mAbValine-AlanineCleavable (enzymatically)Pyrrolobenzodi-azepine (PBD)(Mullard, 2021)