Table 1.
Comparison of RC-48 with T-DM1 and DS-8201 in structure.
| ADC | Kadcyla (T-DM1) | Enhertu (DS-8201) | Disitamab vedotin (RC-48) | |
|---|---|---|---|---|
| Antibody | trastuzumab | Trastuzumab | Hertuzumab | |
| Linker | Name | SMCC | BC-GGFG-OH | MC-VC-PAB |
| Conjugate method | Heterogeneous binding | Site-specific conjugate | Site-specific conjugate | |
| Cleavable | No | Yes | Yes | |
| DAR | 3.5:1 | 8:1 | 4:1 | |
| payload | Released payload | mertansine (DM-1) | Deruxtecan (Dxd) | Monomethyl auristatin E (MMAE) |
| Target | microtubule inhibitor | Topoisomerase I inhibitor | microtubule inhibitor | |
| bystander killing effect | No | Yes | Yes |
ADC: antibody-drug conjugates; DAR: drug/antibody ratio; SMCC: a non-cleavable small maleimidomethyl cyclohexane-1-carboxylate; BC-GGFG-OH: tert-butoxycarbonyl -glycyl glycyl phenylalanyl Glycine; MC-VC-PAB is a cathepsin cleavable ADC linker.