Pharmacokinetics of a long-lasting anti-VEGF fusion protein in rabbit

KH902 suppresses high glucose‐induced migration and sprouting of human retinal endothelial cells by blocking VEGF and PIGF

“…By design, KH902 consists of binding elements taken from the extracellular domain 2 of VEGFR‐1 and the extracellular domain 3 and domain 4 of VEGFR‐2, and is supposed to bind free VEGF/PlGF and then block VEGF/PlGF‐induced angiogenesis. The study of pharmacokinetics of KH902 in rabbit indicates that VEGF concentration in retina and choroid‐RPE declines to nearly half of the baseline 6 h after the intravitreal administration of KH902 . Our study indicated that KH902 could decrease the levels of free VEGF165 and PlGF, and KH902 might have higher effects on anti‐angiogenesis than Avastin.…”

Advances in pharmacotherapy for wet age-related macular degeneration

“…Two preclinical trials to investigate the role of KH902 on experimental CNV in monkeys models found similar results of safety and efficacy [56,57]. Li H et al found that intravitreal administration of KH902 in rabbits showed a good systemic tolerance and a good pharmacokinetic profile, with a rapid distribution from the vitreous into target tissues and duration over 81 days, much longer than that of currently used anti-VEGF compounds [58]. After positive Phase I and Phase II studies results [59][60][61], a Phase III clinical trial (PHOENIX study) was designed to confirm the efficacy and safety of multiple intravitreal injection of KH902 in treatment-naive patients (n = 124) with wet AMD by comparing injections of KH902 with sham-injections.…”

Investigational drugs for retinal vein occlusion

“…Conbercept also blocks all isoforms of VEGF-A, VEGF-B, VEGF-C, and placental growth factor [41,42] and has a higher binding affinity than aflibercept. The 105-patient Aurora Phase II trial of Conbercept in neovascular AMD showed good tolerability and safety and a promising degree of visual improvement.…”