| Generic name | Brand Name | Rightsholder | Disease Area/Indication | Target | Linker | Payload | DAR |
| Gemtuzumab ozogamicin | Mylotarg® | Pfizer Wyeth | CD33-positive acute myeloid leukemia (AML) | CD33 | N-acetyl-γ-calicheamicin | Acid-labile 4-(4-acetylphenoxy)butanoic acid (AcBut) linker | 2 – 3 |
| Brentuximab vedotin | Adcetris® | Pfizer Seagen | CD30-positive lymphomas, including relapsed/refractory Hodgkin lymphoma (cHL), systemic anaplastic large cell lymphoma (sALCL), and cutaneous T-cell lymphoma | CD30 | Monomethyl auristatin E (MMAE) | A protease-cleavable dipeptide linker (valine-citrulline) | 4 |
| Trastuzumab emtansine | Kadcyla® | Genentech Roche | HER2-positive early and metastatic breast cancer, and or as a monotherapy for metastatic disease. | HER2 | DM1, mertansine | A stable, non-reducible thioether linker, SMCC (N-succinimidyl-4-(N-maleimidomethyl) cyclohexane-1-carboxylate) | 3.53 ± 0.05 |
| Inotuzumab ozogamicin | Besponsa® | Pfizer Wyeth | CD22- positive relapsed or refractory (R/R) CD22-positive B-cell acute lymphoblastic leukemia (ALL) in adults and pediatric patients | CD22 | N-acetyl-γ-calicheamicin | An acid-cleavable bifunctional linker | 6 |
| Polatuzumab vedotin | Polivy® | Genentech Roche | Previously untreated DLBCL and relapsed/refractory DLBCL | CD79 | Monomethyl auristatin E (MMAE) | A protease-cleavable peptide Valine-citrulline (VC) linker. | 3.50 |
| Enfortumab vedotin | Padcev® | Pfizer Astellas | Locally advanced or metastatic urothelial cancer | Nectin-4 | Monomethyl auristatin E (MMAE) | A protease-cleavable maleimidocaproyl valine-citrulline (mc-vc-PABC) linker | 3.8 |
| Trastuzumab deruxtecan | Enhertu® | Daiichi Sankyo AstraZeneca | HER2-expressing advanced or metastatic cancers, including breast, gastric, and non-small cell lung cancer (NSCLC). It is indicated for HER2-positive (IHC 3+ or IHC 2+/ISH+) cancers that have progressed after previous treatments. | HER2 | Dxd, exatecan derivative | A stable, cleavable tetrapeptide-based linker (GGFG – glycine-glycine-phenylalanine-glycine) | 7–8 (or ~8) |
| Sacituzumab govitecan | Trodelvy® | Gilead Sciences | Advanced solid tumors, primarily metastatic triple-negative breast cancer (mTNBC) after two or more prior therapies, and metastatic hormone receptor-positive/HER2-negative (HR+/HER2-) breast cancer. It also has accelerated approval for locally advanced or metastatic urothelial carcinoma. | Trop-2 | SN38 | A hydrolyzable linker | 7–8 (or ~8) |
| Belantamab mafodotin | Blenrep® | GSK | Relapsed or refractory multiple myeloma (RRMM) | BCMA | Monomethyl auristatin E F (MMAF) | a non-cleavable maleimidocaproyl (mc) linker | 4 |
| Loncastuximab tesirine | Zynlonta® | ADC Therapeutics | Adult patients with relapsed or refractory (r/r) large B-cell lymphoma, including diffuse large B-cell lymphoma (DLBCL) | CD19 | Pyrrolobenzodiazepine (PBD) dimer SG3199 | Cathepsin-cleavable valine-alanine dipeptide linker | 2.3 |
| Tisotumab vedotin | Tivdak® | Pfizer Genmab | Recurrent or metastatic cervical cancer that has progressed on or after chemotherapy | Tissue factor (TF) | Monomethyl auristatin E (MMAE) | A protease-cleavable valine-citrulline linker | 4 (or ~4.1–4.2) |
| Disitamab vedotin * | Aidixi® | RemeGen | Urothelial carcinoma (bladder cancer) and gastric cancer, particularly in patients with high HER2 expression. It is also actively investigated for breast cancer (including HER2-low) and shows potential in other cancers like lung adenocarcinoma | HER2 | Monomethyl auristatin E (MMAE) | A cleavable maleimidocaproyl-valyl -citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) linker | 3.5–4.5 (or ~4) |
| Mirvetuximab soravtansine | Elahere® | AbbVie | FRα-positive, platinum-resistant epithelial ovarian, fallopian tube, or primary peritoneal cancer who have received prior therapies. It is also being investigated for platinum-sensitive ovarian cancer | FRα | DM4, maytansinoid | A cleavable, sulfo-SPDB, linker | 3.5 (~ 3.3- 4) |
| Sacituzumab tirumotecan | Jiatailai® | Kelun Biotech Merck & Co | Advanced or metastatic solid tumors, with significant clinical development in EGFR-mutated non-small cell lung cancer (NSCLC), triple-negative breast cancer (TNBC), gastric cancer, and urothelial carcinoma. It has shown efficacy in heavily pre-treated patients, including those with TKI-resistant NSCLC | Trop2 | Belotecan-derivative (KL610023) | A hydrolyzable methyl sulfonyl pyrimidine linker | 7.4 |
| Datopotamab deruxtecan | Datroway® | Daiichi Sankyo AstraZeneca | Advanced solid tumors, primarily breast and lung cancers. It is approved for HR-positive/HER2-negative metastatic breast cancer and tested for metastatic triple-negative breast cancer (TNBC) and non-small cell lung cancer (NSCLC). | Trop2 | Dxd, exatecan derivative | A stable, tumor-selective, cleavable tetrapeptide-based linker | 4 |
| * Not approved by the US Food and Drug Administration in the United States | |||||||
