Table 2.
Structural, pharmacodynamic, and pharmacokinetic properties of commonly used antiangiogenic drugs
| Agent | Structure | Target (s) | Mol. weight (kDa) | Fc portion | Affinity (Kd, pM) | Potency (IC50, pM) | t1/2 (vitreous, days) | t1/2 (plasma, days) | Dose |
|---|---|---|---|---|---|---|---|---|---|
| Bevacizumab | Humanized monoclonal full-length antibody | VEGF-A | 149 | Yes | 58–4456 | 500–1476 | 6/7–10 | 21 | 1.25 mg (0.05 mL) |
| Ranibizumab | Humanized recombinant Fab | VEGF-A | 48 | No | 9.2–179 | 88–1140 | 7.1 | 0.25 | 0.5 mg (0.05 mL) |
| Aflibercept | Recombinant fusion protein | VEGF-A, VEGF-B, PlGF | 115 | Yes | 0.49–9263 | 16–90 | 4.5–4.7 (rabbits) | 18 | 2 mg (0.05 mL) |
| Brolucizumab | Humanized single-chain antibody fragment | VEGF-A | 26 | No | 28.4 (for VEGF₁₆₅) | 860 | 4.4–5.6 | 6 | 6 mg (0.05 mL) |
| Faricimab | Bispecific monoclonal antibody | VEGF-A, Ang-2 | 150 | Modified Fc region to reduce FcγR and FcRn binding | 46–60 (VEGF-A), 22–30 (Ang-2) | 490 (VEGF-A), 240 (Ang-2) | 6.7–12 | 12 | 6 mg (0.05 mL) |
Abbreviations: VEGF Vascular endothelial growth factor, PlGF placental growth factor, Ang-2 Angiopoietin-2, Fab fragment antigen-binding, Fc fragment crystallisable, FcγR Fc gamma receptor, FcRn neonatal Fc receptor, Kd dissociation constant (affinity), IC₅₀ half maximal inhibitory concentration (potency), t1/2 half-life