Comparison between first-, second-, and third-generation ADCs
| Properties/Generation | First-generation ADCs | Second-generation ADCs | Third-generation ADCs |
|---|---|---|---|
| Antibody type | Murine or chimeric antibodies | Human-mouse chimeric antibodies, humanized monoclonal antibodies | Fully human monoclonal antibodies |
| Linker | Unstable | Cleavable and non-cleavable | More stable, site-specific |
| Cytotoxin | Lower toxicity | Higher toxicity | Various highly effective small molecule toxins |
| Drug-to-antibody ratio | Non-uniform | Non-uniform | Uniform |
| Targeting | Lower | Higher | Highest |
| Immunogenicity | High | Lower | Lowest |
| Safety | Stronger toxicity/side effects | Stronger side effects | Lower toxicity |
| Clinical efficacy | Poor effect | Better effect | Best effect |
| Clinical application | Few clinical applications | Widespread clinical application | Widespread application with significant effects |
| Features | Non-site-specific conjugation, short half-life | Site-specific conjugation, improved efficacy | Site-specific conjugation, wider therapeutic window |
ADCs, antibody-drug conjugates.