Table 1.
Drug | Structure | Target | Standard Dose | FDA-Approved Clinical Indications | Landmark Clinical Trials | FDA Approval Date |
---|---|---|---|---|---|---|
Pegaptanib | 28 nucleotide RNA aptamer with a 5’-attachment of polyethylene glycol | VEGF-A165 | 0.3 mg/0.09 mL | AMD | AMD: VISION [62] | 2004 |
Bevacizumab | Recombinant humanized monoclonal IgG1 antibody | All isoforms of VEGF-A | 1.25 mg/0.05 mL | Off-label for ophthalmic use |
AMD: CATT [71] DME: BOLT [69], BEVORDEX [70] |
Off-label for ophthalmic use |
Ranibizumab | Recombinant humanized monoclonal IgG1 kappa antibody fragment | All isoforms of VEGF-A | 0.3 mg/0.05 mL or 0.5 mg/0.05 mL | AMD, DR, DME, ME due to RVO, myopic choroidal neovascularization |
AMD: MARINA [81], ANCHOR [82] DME: RISE, RIDE [48] RVO: BRAVO, CRUISE [51] |
2006 |
Aflibercept | Soluble decoy receptor comprised of an Fc fragment of IgG1 fused to binding domains of VEGFR-1 and VEGFR-2 | All isoforms of VEGF-A, VEGF-B, and placental growth factor | 2.0 mg/0.05 mL | AMD, DR, DME, ME due to RVO, retinopathy of prematurity |
AMD: VIEW 1, VIEW 2 [90] DME: VISTA, VIVID [91] RVO: COPERNICUS, GALILEO [92] |
2011 |
Brolucizumab | Humanized monoclonal single-chain variable fragment (scFv) | All isoforms of VEGF-A | 6.0 mg/0.05 mL | AMD, DME |
AMD: HAWK, HARRIER [98] DME: KESTREL, KITE [102] |
2019 |
Faricimab | IgG1-derived bispecific monoclonal antibody | Angiopoietin-2 and all isoforms of VEGF-A | 6.0 mg/0.05 mL | AMD, DME |
AMD: TENAYA, LUCERNE [108] DME: RHINE, YOSEMITE [109] |
2022 |