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. Author manuscript; available in PMC: 2018 Jan 1.
Published in final edited form as: Handb Exp Pharmacol. 2017;242:271–307. doi: 10.1007/164_2016_78

Table 1.

Current VEGF/KDR (kinase-insert-domain-containing receptor) anti-angiogenic targets in clinical trials

Drug Drug target Disease target Clinicaltrials.gov ID Phase Number patients Relevant clinical study
Pazopanib VEGFR tyrosine kinase inhibitor AMD NCT00612456


NCT01134055
    2,
Completed 2009
    2b
  70


510
Danis R, et al. Br J Ophthalmol 2014;98:172–178
TG100801 VEGF tyrosine kinase inhibitor AMD, PDR NCT00414999     1,
Completed
  44
TG100801 Same AMD NCT00509548     2,
Terminated early
Terminated after 7 due to corneal deposits
OPT-302 VEGFR-3 AMD NCT02543229     1 Enrolling 50
Regorafenib Receptor tyrosine kinase VEGFR2-TIE2 AMD NCT02222207     2   52
rAAV.sFlt-1 Flt1 AMD NCT01494805     1 and 2   40 Rakoczy EP, et al. Lancet. 2015;386(10011):2395–403.
PAN-90806 Anti-VEGFR AMD NCT02022540     1   50
Squalamine lactate VEGF AMD
RVO
PDR
NCT01678963
NCT02614937
NCT01769183
    2
    1 and 2
    2
142
  20
    6
Abicipar Pegol (AGN-150998) Anti-VEGF AMD


DME
NCT01397409
NCT02181517
NCT02181504
NCT02462928
NCT02186119
    2
    2
    2
    3
    2
271
  25
  25
900, R
151
PF582 Anti-VEGF AMD NCT02121353     1 and 2   25
EYE001 Anti-VEGF Pegylated Aptamer AMD NCT00021736     2 and 3 540
AL-39324 Inhibit VEGFR and PDGFR AMD NCT00992563     2   35
LHA510 VEGFA-inhibitor AMD NCT02076919
NCT02355028
    1
    2

135
X-82 VEGF and PDGF inhibitor AMD NCT02348359
NCT01674569
    2, R
    1 and 2
132
  35
ESBA1008 Anti-VEGF AMD NCT01304693     1 and 2 376
BCD-021 Anti-VEGF AMD NCT02450981     1   10
LMG324 Anti-VEGF AMD NCT02398500     1 and 2  25, Terminated
TK001 Anti-VEGF AMD NCT02613559     1  27,R
ORA102 AMD NCT00745511     1 and 2   96
RG7716 Anti-VEGFA AMD NCT02484690     2 271
AGN211745 VEGFR-1 siRNA AMD NCT00395057     2 138, Terminated
PTK787 (Vatalanib) Tyrosine kinase inhibitor targets VEGFR AMD NCT00138632     1 and 2   50

Abbreviations: R= recruiting; AMD = neovascular age-related macular degeneration; DME = diabetic macular edema; PDR = proliferative diabetic retinopathy; RVO = retinal vein occlusion