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. 2022 Dec 29;15(1):122. doi: 10.3390/pharmaceutics15010122

Table 1.

Anti-VEGF therapies in diabetic macular edema and diabetic retinopathy.

Drug Mechanism of Action Dose Gain in Letters in DME Change in DR Studies
Pegaptanib Pegylated oligoribonucleotide (aptamer), binds to VEGF165 0.3 mg q6 1 year: +5.2
2 year: +6.1
Reduction of NV in eight out of 19 patients [18,19]
Bevacizumab Humanized murine full-length mAb, binds VEGF-A alone 1.25 mg 1 year (20/32–20/40): +7.5
1 year (20/50–20/320): +11.8
2 year (20/32–20/40): +6.8
2 year (20/50–20/320): +13.3
2 years: 30% improvement * [20]
Ranibizumab Humanized murine mAb fragment, binds VEGF-A, higher affinity 0.3 mg
0.5 mg
1 year (20/32–20/40): +8.3
1 year (20/50–20/320): +14.2
2 year (20/32–20/40): +8.6
2 year (20/50–20/320): +16.1
2 years: 38% improvement *
Less visual field lost at 5 years vs PRP
[14,20]
Aflibercept Human fusion protein of the IgG Fc region,
binds
VEGF-A, VEGF-B, PlGF-1 and PlGF-2
2.0 mg q8 1 year (20/32–20/40): +8.0
1 year (20/50–20/320): +18.9
2 year (20/32–20/40): +7.8
2 year (20/50–20/320): +18.1
2 years: 70% improvement
2 years: 62% improvement
33% need of vitrectomy
[20,21,22,23]
Conbercept Recombinant fusion protein,
Binds VEGF-A, -B, and PlGF
0.5 mg 1 year: +8.6
Laser crossover
No RCT
Improvement in NV severity
[24]
Brolucizumab Single-chain antibody fragment (scFv) with high affinity for VEGF 6 mg q6-q12 dosing 50–55% • 1 year: +9.2 and +10.6 29.6% improvement * [25]
Faricimab Bispecific antibody
Inhibit Ang-2 and VEGF-A
6 mg
>70% achieved q12 in T&E
YOSEMITE 1 year:
+10.7 q8
+11.8 PTI
RHINE 1 year:
+11.8 q8
+10.8 PTI
YOSEMITE 1 year: 46% q8
42.5% PTI
RHINE 1 year:
44.2% q8
43.7% PTI
[26]

NV: neovascularization; PTI: personalized treatment interval (YOSEMITE and RHINE); RCT: randomized controlled trial; * Improvement from baseline: ETDRS diabetic retinopathy severity scale level improved by at least two levels or there was complete regression of active proliferative diabetic retinopathy (PDR). • probability of q12 dosing posterior to loading phase through week 52.