Table 1.
A list of worldwide antibody–drug conjugates that have been approved for clinical use (as of August 2023, in a reverse chronological order of their approval dates)
| ADC Name (developing company) | Antigen | Linker | Payload | Target | Approval office (approved date) | Approved disease indications |
|---|---|---|---|---|---|---|
| Mirvetuximab soravtansine (ImmunoGen) | FRα | Sulfo-SPDB (cleavable) | DM4 | DNA (human) | U.S. FDA (Nov, 2022) | FRα-positive epithelial ovarian cancer |
| Tisotumab vedotin (Seagen) | TF | Mc-Val-Cit-PABC (cleavable) | MMAE | Microtubule (human) | U.S. FDA (Sep, 2021) | Recurrent or metastatic cervical cancer |
| Disitamab vedotin (RemeGen) | HER2 | Mc-Val-Cit-PABC (cleavable) | MMAE | Microtubule (human) | China NMPA (Jun, 2021) | Advanced or metastatic gastric cancer |
| Loncastuximab tesirine (ADC Therapeutics) | CD19 | Mal-PEG8-Val-Ala- PABC (cleavable) | SG3199 | DNA (human) | U.S. FDA (Apr, 2021) | Relapsed or refractory large B-cell lymphoma |
| Cetuximab sarotalocan (Rakuten Medical) | EGFR | Linear alkyl/alkoxy linker (uncleavable) | IRDye 700DX | not available | Japan PMDA (Sep, 2020) | Advanced or recurrent head and neck cancer |
| Belantamab mafodotin (GlaxoSmithKline) | BCMA | Maleimido-caproyl (uncleavable) | MMAF | Microtubule (human) | U.S. FDA (Aug, 2020) | Relapsed or refractory multiple myeloma |
| Sacituzumab govitecan (Gilead Sciences) | TROP2 | CL2A (cleavable) | SN38 | TOP1 (human) | U.S. FDA (Apr, 2020) | Metastatic triple-negative breast cancer |
| Enfortumab vedotin (Astellas) | Nectin-4 | Mc-Val-Cit-PABC (cleavable) | MMAE | Microtubule (human) | U.S. FDA (Dec, 2019) | Advanced or metastatic urothelial cancer |
| Trastuzumab deruxtecan (Daiichi Sankyo) | HER2 | Mc-Gly-Gly-Phe- Gly (cleavable) | DXd | TOP1 (human) | U.S. FDA (Dec, 2019) | Unresectable HER2-positive breast cancer |
| Polatuzumab vedotin (Roche) | CD79b | Mc-Val-Cit-PABC (cleavable) | MMAE | Microtubule (human) | U.S. FDA (Jun, 2019) | Diffuse large B-cell lymphoma |
| Moxetumomab pasudotox (AstraZeneca) | CD22 | Mc-Val-Cit-PABC (cleavable) | PE38 | EEF2K (human) | U.S. FDA (Sep, 2018) | Relapsed or refractory hairy cell leukemia |
| Inotuzumab ozogamicin (Pfizer) | CD22 | AcButDMH (cleavable) | N-acetyl-γ-calicheamicin | DNA (human) | U.S. FDA (Aug, 2017) | B-cell precursor acute lymphoblastic leukemia |
| Trastuzumab emtansine (Roche) | HER2 | SMCC (uncleavable) | DM1 | Microtubule (human) | U.S. FDA (Feb, 2013) | HER2-positive metastatic breast cancer |
| Brentuximab vedotin (Seagen) | CD30 | Mc-Val-Cit-PABC (cleavable) | MMAE | Microtubule (human) | U.S. FDA (Aug, 2011) | Hodgkin lymphoma; Large-cell lymphoma |
| Gemtuzumab ozogamicin (Pfizer) | CD33 | AcButDMH (cleavable) | N-acetyl-γ-calicheamicin | DNA (human) | U.S. FDA (Mar, 2000) | CD33-positive acute myeloid leukemia |
AcButDMH: AcBut acyl hydrazonedisulfide; BCMA: B-cell maturation antigen; CD19: B-lymphocyte antigen CD19; CD22: B-cell receptor CD22; CD30: lymphocyte activation antigen CD30; CD33: myeloid cell surface antigen CD33; CD79b: immunoglobulin-associated beta; DM1: derivative of maytansine 1; DM4: derivative of maytansine 4; DXd: DX-8951 derivative; EEF2K: eukaryotic elongation factor 2 kinase; EGFR: epidermal growth factor receptor; TF: tissue factor; FRα: folate receptor alpha; HER2: human epidermal growth factor receptor 2; Mc-Gly-Gly-Phe-Gly: maleimidocaproyl-glycine-phenylalanine-glycine- glycine; Mc-Val-Cit-PABC: maleimidocaproyl-valine-citrulline-p-aminobenzoyloxycarbonyl; MMAE: monomethyl auristatin-E; MMAF: monomethyl auristatin-F; Nectin-4: Nectin cell adhesion molecule 4; PE38: 38kD fragment of Pseudomonas exotoxin A; SMCC: succinimidyl‐4‐(N‐maleimidomethyl)cyclohexane‐1‐carboxylate; SN38: active metabolite of irinotecan; Sulfo-SPDB: sulfonyl-N-succinimidyl 4-(2-pyridyldithio) butyrate; TOP1: DNA topoisomerase 1; TROP2: tumor-associated calcium signal transducer 2.
The approved administrations/offices included: U.S. Food and Drug Administration (U.S. FDA), National Medical Products Administration of China (China NMPA) and Pharmaceuticals and Medical Devices Agency of Japan (Japan PMDA).