Table 2 Pharmacological properties of anti-HER2 ADCs undergoing clinical trials
| ADC name | Ab | Linker | Payload | DAR | Ongoing clinical trialsa |
|---|---|---|---|---|---|
| SYD985 | Trastuzumab |
Valine-citrulline linker (cleavable) | Seco-DUBA (DNA-alkylating) | 2.8 | NCT03262935 NCT04602117 NCT04235101 NCT01042379 |
| ZW49 | ZW25 | Cleavable |
N-acyl sulfonamide auristatin (microtubule inhibitor) | N.A. | NCT03821233 |
| PF-06804103 | Trastuzumab-derived Ab | Maleimidocaproyl-valine-citrulline linker (cleavable) | Aur-06380101 | 4 | NCT03284723 |
| MRG002 | Anti-HER2 IgG1 | N.A. | Monomethyl auristatin E | NA |
CTR20181778 NCT04492488, NCT04742153 |
| GQ1001 | Anti-HER2 IgG | NA | NA | NA | NCT04450732 |
| ARX788 | Modified heavy chain Ala114 of anti-HER2 mAb |
Amberstatin (AS269) (non-cleavable) | Dolastatin monomethyl auristatin F (microtubule inhibitor) | 1.9 | NCT03255070 |
| A166 | Trastuzumab | Valine citrulline peptide (cleavable linker) | Duostatin-5 (microtubule inhibitor) | N.A. | NCT03602079 |
| XMT-1522 | HT-19 (anti-HER2 IgG1) | Cleavable hydrophilic polymer | AF-HPA (microtubule inhibitor) | 12 | NCT02952729 |
| RC48-ADC | Hertuzumab (anti-HER2 humanized Ab) | Valine citrulline peptide (cleavable linker) | Monomethyl auristatin E (microtubule inhibitor) | 4 |
NCT04329429 NCT04280341 NCT04311034 NCT04714190 NCT04073602 NCT04264936 NCT03556345 NCT03500380 NCT03052634 |
| BDC-1001 | Trastuzumab | Non cleavable linker | TLR7/8 inhibitor | NA | NCT04278144 |
| FS-1502 | Trastuzumab | NA | Monomethyl Auristatin F | NA | NCT03944499 |
| GQ1001 | NA | NA | NA | NA | NCT04450732 |
| ALT-P7 | Trastuzumab biobetter HM2 | Cysteine-containing peptide |
Monomethyl auristatin E (microtubule inhibitor) | NA | NCT03281824 |