Table 1.
Representative native ADCs using site-specific conjugation methods that are currently in phase 1 clinical trials for cancer therapy [44, 95, 111, 112]
| Chemistry | Name | Developer | Drug to antibody ratio | Description | Clinical trial identifier |
|---|---|---|---|---|---|
| TGase-glutamine | PF-06664178 | Pfizer | 2 | • Anti-TROP2 IgG1 • Valine-citrulline cleavable linker • Auristatin-based cytotoxic payload |
NCT02122146 |
| Glycan remodeling | ADCT-601 | ADC Therapeutics | 2 | • Anti-Human AXL IgG1 • Valine-citrulline cleavable linker • PBD (pyrrolobenzodiazepine)—cytotoxic dimer payload |
NCT03700294 |
| XMT-1592 | Mersana Therapeutics | 6 | • Anti-NaPi2b IgG1 • Proprietary platform (Dolasynthen) • Auristatin-based cytotoxic payload |
NCT04396340 | |
| ThioBridge | OBI-999 | OBI-Pharmaceuticals | 4 | • Anti-Globo H IgG • Proteolytically cleavable linker • Auristatin-based cytotoxic payload |
NCT04084366 |