| Year | ADC | Target | Cancer Type | Remarks |
| 2000 | Gemtuzumab ozogamicin (Mylotarg) | CD33 | Acute myeloid leukemia (AML) | Discontinued in 2010, reapproved in 2017. |
| 2011 | Brentuximab vedotin (Adcetris) | CD30 | Anaplastic large cell lymphoma (ALCL), Hodgkin lymphoma, systemic anaplastic large cell lymphoma (sALCL), cutaneous T-cell lymphoma (CTCL) | |
| 2013 | Ado-trastuzumab emtansine (Kadcyla) | HER2 | Breast cancer, gastric cancer, metastatic urothelial carcinoma | |
| 2017 | Inotuzumab ozogamicin (Besponsa) | CD22 | B-cell acute lymphoblastic leukemia (ALL) | |
| 2017 | Gemtuzumab ozogamicin (Mylotarg) | CD33 | Acute myeloid leukemia (AML) | |
| 2018 | Moxetumomab pasudotox (Lumoxiti) | CD22 | Hairy cell leukemia (HCL) | |
| 2019 | Polatuzumab vedotin-piiq (Polivy) | CD79b | Diffuse large B-cell lymphoma (DLBCL) | |
| 2019 | Enfortumab vedotin (Padcev) | Nectin-4 | Urothelial carcinoma | |
| 2019 | Trastuzumab deruxtecan (Enhertu) | HER2 | Breast cancer, gastric cancer | |
| 2020 | Sacituzumab govitecan (Trodelvy) | Trop-2 | Metastatic triple-negative breast cancer (mTNBC), metastatic urothelial carcinoma | |
| 2021 | Belantamab mafodotin-blmf (Blenrep) | BCMA | Multiple myeloma | |
| 2021 | Loncastuximab tesirine-lpyl (ZYNLONTA) | CD19 | Diffuse large B-cell lymphoma (DLBCL), high-grade B-cell lymphoma (HGBL), primary mediastinal large B-cell lymphoma (PMBCL) | |
| 2021 | Tisotumab vedotin-tftv (Tivdak) | Trop-2 | Recurrent or metastatic cervical cancer | |
| 2022 | Mirvetuximab soravtansine (ELAHERE) | Folate receptor alpha (FRĪ±) | Ovaian cancer, fallopian tube cancer, primary peritoneal cancer | Discontinued in August 2023 due to commercial considerations. |
| 2023 | Tesetaxel (Padcev T) | Trop-2 | Metastatic urothelial carcinoma (mUC) | |
| 2023 | Tucatinib-trastuzumab vedotin (T-DXd) | HER2 | Metastatic breast cancer |