Comparison of key attributes of 22-20, 20-22, 20-20, v-mab, rituximab (r-mab), and e-mab
| Attribute . | 22-20 . | 20-22 . | 20-20 . | v-mab . | r-mab . | e-mab . |
|---|---|---|---|---|---|---|
| Size, kDa | 365 | 365 | 365 | 150 | 150 | 150 |
| Valency | ||||||
| CD20 | 4 | 2 | 6 | 2 | 2 | 0 |
| CD22 | 2 | 4 | 0 | 0 | 0 | 2 |
| Rapid internalization | No | Yes | No | No | No | Yes |
| Off-rate* (Raji) | 0.54 | 0.95 | 0.36 | 1.0 | 2.5† | ND |
| In vitro growth inhibition (EC50, nM) | ||||||
| Daudi | 0.33 | 0.5 | 0.15‡ | > 15 (+GAH = 1.7) | > 15 | None |
| Raji | 0.32 | 3.5 | 0.07‡ | > 15 (+GAH = 1.0) | > 15 | None |
| Ramos | 0.20 | 1.6 | 0.15‡ | > 15 (+GAH = 0.5) | > 15 | None |
| B-cell depletion | Moderate | Moderate | Moderate | Strong | Strong† | Moderate |
| Apoptosis (Daudi, % annexin+) | ||||||
| −GAH | 23.2 | 25.5 | 16.9 | 10.6 | 17.7 | 13.7 |
| +GAH | ND | ND | ND | 14.0 | 16.0 | ND |
| Ca2+ mobilization | ||||||
| −GAH | None | None | None‡ | None‡ | None‡ | None |
| +GAH | Weak | Weak | Weak‡ | Moderate‡ | Moderate‡ | None |
| CDC | No | No | No‡ | Yes | Yes | No |
| ADCC | Moderate | Strong | Strong‡ | Strong | Strong | Weak |
| Trafficking to lipid rafts | ||||||
| CD22 | Enhanced | Enhanced | No | No | No | Yes |
| CD20 | Yes | Yes | Yes | Yes | Yes | No |
| Homotypic adhesion | Strong | Strong | Moderate | No | No | No |
| Serum stability§ | 5 days§ | 5 days§ | 11 days‖ | 11 days‖ | ND | ND |
| Attribute . | 22-20 . | 20-22 . | 20-20 . | v-mab . | r-mab . | e-mab . |
|---|---|---|---|---|---|---|
| Size, kDa | 365 | 365 | 365 | 150 | 150 | 150 |
| Valency | ||||||
| CD20 | 4 | 2 | 6 | 2 | 2 | 0 |
| CD22 | 2 | 4 | 0 | 0 | 0 | 2 |
| Rapid internalization | No | Yes | No | No | No | Yes |
| Off-rate* (Raji) | 0.54 | 0.95 | 0.36 | 1.0 | 2.5† | ND |
| In vitro growth inhibition (EC50, nM) | ||||||
| Daudi | 0.33 | 0.5 | 0.15‡ | > 15 (+GAH = 1.7) | > 15 | None |
| Raji | 0.32 | 3.5 | 0.07‡ | > 15 (+GAH = 1.0) | > 15 | None |
| Ramos | 0.20 | 1.6 | 0.15‡ | > 15 (+GAH = 0.5) | > 15 | None |
| B-cell depletion | Moderate | Moderate | Moderate | Strong | Strong† | Moderate |
| Apoptosis (Daudi, % annexin+) | ||||||
| −GAH | 23.2 | 25.5 | 16.9 | 10.6 | 17.7 | 13.7 |
| +GAH | ND | ND | ND | 14.0 | 16.0 | ND |
| Ca2+ mobilization | ||||||
| −GAH | None | None | None‡ | None‡ | None‡ | None |
| +GAH | Weak | Weak | Weak‡ | Moderate‡ | Moderate‡ | None |
| CDC | No | No | No‡ | Yes | Yes | No |
| ADCC | Moderate | Strong | Strong‡ | Strong | Strong | Weak |
| Trafficking to lipid rafts | ||||||
| CD22 | Enhanced | Enhanced | No | No | No | Yes |
| CD20 | Yes | Yes | Yes | Yes | Yes | No |
| Homotypic adhesion | Strong | Strong | Moderate | No | No | No |
| Serum stability§ | 5 days§ | 5 days§ | 11 days‖ | 11 days‖ | ND | ND |
GAH indicates goat anti–human Fc crosslinking antibody; and ND, not done.
Off-rate shown as the quotient of the T1/2 of the test article divided by T1/2 of v-mab.
Data from Goldenberg et al.31
Data from Rossi et al.9
No change from day 0 by bispecific ELISA.
A total of 85% compared with day 0 by ELISA.