Table 1.
All compounds introduced in this perspective review.
| # | Administrated Drug | Formulation | Cancer Antigen | Disease | Vector | Payload | Linker | Status | References |
|---|---|---|---|---|---|---|---|---|---|
| (1) | Anti-HER2 bispecific mAb | Anti-HER2 bispecific mAb targeting two non-overlapping epitopes on HER2 | HER2 | - | Anti-HER2 bispecific mAb | - | - | Basic research | [15] |
| (2) | Sym004 | The mixture of two anti-EGFR mAbs | EGFR | - | anti-EGFR mAb | - | - | Basic research | [16] |
| (3) | Nivolumab (Opdivo®) | Anti-PD-1 mAb | PD-1 | Metastatic lung squamous cell carcinoma | - | Nivolumab | - | Launched in 2014 | [17] |
| (4) | Isatuximab (Sarclisa®) | Anti-CD38 mAb | CD38 | Multiple myeloma | - | Isatuximab | - | Launched in 2020 | [18] |
| (5) | Tafasitamab (Monjuvi®) | Anti-CD19 mAb | CD19 | Diffuse large B cell lymphoma | - | Tafasitamab | - | Launched in 2020 | [18] |
| (6) | Naxitamab (Danyelza®) | Anti-GD2 mAb | GD2 | High-risk neuroblastoma and refractory osteomedullary disease | - | Naxitamab | - | Launched in 2020 | [18] |
| (7) | Dostarlimab (Jemperli®) | Anti-PD-1 mAb | PD-1 | Endometrial cancer | - | Dostarlimab | - | Launched in 2021 | [18] |
| (8) | Gemtuzumab ozogamicin (Mylotarg®) | Anti-CD33 ADC with N-acetyl-γ-calicheamicin | CD33 | Blood cancer | Gemtuzumab | N-acetyl-γ-calicheamicin | Acid-cleavable linker | Launched in 2000 and 2017 | [19] |
| (9) | Brentuximab vedotin (Adcetris®) | Anti-CD30 ADC with MMAE | CD30 | Blood cancer | Brentuximab | MMAE | Enzymatically cleavable linker | Launched in 2011 | [20,21,22] |
| (10) | Adotrastuzumab emtansine (Kadcyla®) | Anti-HER2 ADC with DM1 | HER2 | Breast cancer | Adotrastuzumab | DM1 | Uncleavable linker | Launched in 2013 | [23,24] |
| (11) | Inotuzumab ozogamicin (Besponsa®) | Anti-CD22 ADC with N-acetyl-γ-calicheamicin | CD22 | Blood cancer | Inotuzumab | N-acetyl-γ-calicheamicin | Acid-cleavable linker | Launched in 2017 | [25] |
| (12) | Moxetumomab pasudotox-tdfk (Lumoxiti®) | Anti-CD22 ADC with PE38 | CD22 | Blood cancer | Moxetumomab | PE38 | Reductively cleavable linker | Launched in 2018 | [26] |
| (13) | Polatuzumab vedotin-piiq (Polivy®) | Anti-CD79b ADC with MMAE | CD79b | Blood cancer | Polatuzumab | MMAE | Enzymatically cleavable linker | Launched in 2019 | [27] |
| (14) | Enfortumab vedotin-ejfv (Padcev®) | Anti-Nectin4 ADC with MMAE | Nectin4 | Urothelial cancer | Enfortumab | MMAE | Enzymatically cleavable linker | Launched in 2019 | [28] |
| (15) | Trastuzumab deruxtecan-nxki (Enhertu®) | Anti-HER2 ADC with DXd | HER2 | Breast cancer | Trastuzumab | DXd | Enzymatically cleavable linker | Launched in 2019 | [29] |
| (16) | Sacituzumab govitecan-hziy (Trodelvy®) | Anti-TROP2 ADC with SN-38 | TROP2 | Breast cancer | Sacituzumab | SN-38 | Acid-cleavable linker | Launched in 2020 | [30,31,32] |
| (17) | Belantamab mafodotin-blmf (Blenrep®) | Anti-BCMA ADC with MMAF | BCMA | Blood cancer | Belantamab | MMAF | Uncleavable linker | Launched in 2020 | [33] |
| (18) | Loncastuximab tesirine-lpyl (Zynlonta®) | Anti-CD19 ADC with SG3199 | CD19 | Blood cancer | Loncastuximab | SG3199 | Enzymatically cleavable linker | Launched in 2021 | [34] |
| (19) | Tisotumab vedotin-tftv (Tivdak®) | Anti-Tissue Factor ADC withMMAE | Tissue Factor | Cervical cancer | Tisotumab | MMAE | Enzymatically cleavable linker | Launched in 2021 | [35] |
| (20) | Datopotamab deruxtecan (Dato-DXd) | Anti-ROP2 ADC | ROP2 | Solid cancer | Anti-ROP2 mAb | DXd | Linker | Clinical trial | [36] |
| (21) | Patritumab deruxtecan (HER3-DXd) | Anti-HER3 ADC | HER3 | Solid cancer | Anti-HER3 mAb | DXd | Linker | Clinical trial | [37] |
| (22) | DS-7300 | Anti-B7-H3 ADC | B7-H3 | Solid cancer | Anti-HER3 mAb | DXd | Linker | Clinical trial | [38] |
| (23) | DS-6000 | Anti-CDH6 ADC | CDH6 | Solid cancer | Anti-CDH6 | DXd | Linker | Clinical trial | [39] |
| (24) | DS-3939 | Anti-TA-MUC1 ADC | TA-MUC1 | Solid cancer | Anti-TA-MUC1 | DXd | Linker | Clinical trial | [39] |
| (25) | BYON3521 | Anti-c-MET receptor ADC | c-MET receptor | Solid cancer | Anti-c-MET receptor mAb | Duocarmycin | Cathepsin-cleavable linker | Phase1 (NCT05323045) | - |
| (26) | STRO-002 | Anti-folate receptor α ADC | Folate receptor α | Solid cancer | Anti-folate receptor α mAb | 3-Aminophenyl hemiasterlin | Cathepsin-cleavable linker | Phase1 (NCT03748186) | - |
| (27) | STI-6129 | Anti-CD38 ADC | CD38 | Solid cancer | Anti- CD38 mAb | Duostatin 5.2 | Non-polyethylene glycol linker | Phase1 (NCT05584709) | - |
| (28) | ARX788 | Anti-HER2 ADC | HER2 | Solid cancer | Anti-HER2 mAb | MMAF | Non-natural amino acid linker | Phase2 (NCT04983121) | - |
| (29) | MORAb-202 | Anti-folate receptor α ADC | Folate receptor α | Solid cancer | Anti-folate receptor α mAb | Eribulin | Cathepsin-cleavable linker | Phase2 (NCT05577715) | - |
| (30) | SYD985 | Anti-HER2 ADC | HER2 | Solid cancer | Anti-HER2 mAb | Duocarmycin | Cathepsin-cleavable linker | Phase2 (NCT04205630) | - |
| (31) | RC48 (disitamab vedotin) | Anti-HER2 ADC | HER2 | Solid cancer | Anti-HER2 mAb | Auristatin E | Cathepsin-cleavable linker | Phase2 (NCT04329429) | - |
| (32) | MRG002 | Anti-HER2 ADC | HER2 | Solid cancer | Anti-HER2 mAb | MMAE | Cathepsin-cleavable linker | Phase2 (NCT05263869) | - |
| (33) | XMT-1536 (upifitamab rilsodotin) | Anti-NaPi2b ADC | NaPi2b | Solid cancer | Anti-NaPi2b mAb | Auristatin F | Hydrophilic polymer linker | Phase3 (NCT05329545) | - |
| (34) | IMGN-853 (mirvetuximab soravtansine) | Anti-folate receptor α ADC | Folate receptor α | Solid cancer | Anti-folate receptor α mAb | DM4 | Disulfide-containing cleavable linker | Phase3 (NCT04296890) | - |
| (35) | Doxil® | Doxorubicin-encapsulated liposome coated with PEG | - | Ovarian cancer and breast cancer | - | Doxorubicin | - | Launched in 1999 and 2003 | [40,41] |
| (36) | PEG engagerEGFR, Doxisome | Anti-EGFR and anti-PEG bispecific Ab, PEGylated liposomes containing doxorubicin | EGFR | Solid cancer | Anti-EGFR and anti-PEG bispecific Ab | Doxorubicin | - | Basic research | [42] |
| (37) | Anti-HER2 nanobody 11A4 fused to an albumin-binding domain-maleimide-auristatin F | Anti-HER2 nanobody 11A4 fused to an albumin-binding domain with auristatin F | HER2 | Solid cancer | Anti-HER2 nanobody 11A4 | Auristatin F | Maleimide | Basic research | [43] |
| (38) | Anti-transferrin receptor nanobodies with neurotensin | Anti-transferrin receptor nanobodies with neurotensin | - | - | Anti-transferrin receptor nanobodies | Neurotensin | - | Basic research | [44] |
| (39) | Anti-EGFR nanobodies-drug | Anti-EGFR nanobodies with MMAE | EGFR | Solid cancer | Anti-EGFR nanobodies | MMAE | - | Basic research | - |
| (40) | ADC–albumin complex | ADC with or without PEGs | Arbitrary | Solid cancer | Arbitrary | Arbitrary | - | Under analysis in Tashima lab | - |
| (41) | mAb-loaded nanoparticles containing payloads | mAb-loaded nanoparticles containing payloads | Arbitrary | Solid cancer | Arbitrary | Arbitrary | - | Under analysis in Tashima lab | - |