Table 3. Characteristics of the conjugates obtained using different conjugation strategies.
| Conjugation scheme | Conjugate (n° CH2 in the linker) | fVi avMW | Component derivatised (activation degree) | Aminoacids activated on CRM 197 | fVi to CRM197 w/w ratio | fVi to CRM197 molar ratio | % free fVi* | |
|---|---|---|---|---|---|---|---|---|
| Random | 1A | fVi-CRMODH(x = 0) | 43 | CRM197(7 linkers) | Asp/Glu | 0.61 | na | 5.67 |
| fVi-CRMSDH(x = 2) | CRM197(6 linkers) | Asp/Glu | 0.78 | na | 25.2 | |||
| fVi-CRMADH(x = 4) | CRM197(6 linkers) | Asp/Glu | 0.59 | na | <20 | |||
| fVi-CRMPDH(x = 5) | CRM197(9 linkers) | Asp/Glu | 0.46 | na | 0.3 | |||
| 1B | fVi(DMT-MM)CRMADH | CRM197(6 linkers) | Asp/Glu | 0.51 | na | 13.5 | ||
| 1C | fVi(ADH)-CRM197 | fVi(22% RU) | Asp/Glu | 1.63 | na | <20 | ||
| 1D | fViADHN3-CRMalkyne | CRM197(12 linkers) fVi(22.5% RU) |
Lys | 0.34 | na | <20 | ||
| Selective terminal | 1F | fVis(ADH)-CRM197 | 8.6 | fVi(1linker/chain) | Asp/Glu | 0.23 | 1.53 | <20 |
| 1E | fVisSH-CRMSBAP | CRM197(9 linkers) fVi(1 linker/chain) |
Lys | 0.28 | 1.91 | <20 | ||
RU = repeating units, na = not applicable, *no free CRM197 detected in all the conjugates.