Seattle—Results from TIME-2, a phase IIA study, support further development of combination treatment with subcutaneous injection of the Tie2 activator, AKB-9778 (Aerpio Therapeutics), plus intravitreous (IVT) anti-VEGF injection for diabetic macular edema (DME), as well as the development of non-IVT therapy for the treatment of diabetic retinopathy.
Speaking at ARVO 2016, Arshad Khanani, MD, noted that multiple therapeutic approaches to regulate Tie2 activity are under development. AKB-9778 is the only Tie2 targeted compound in clinical trials that has completed a phase II randomized, placebo-controlled study in the setting of retinal disease.
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“TIME-2 provides proof of concept for treatment of diabetic eye disease, both DME and diabetic retinopathy, by activation of Tie2 through inhibition of vascular endothelial-protein tyrosine phosphatase (VE-PTP) mediated by AKB-9778,” said Dr. Khanani, who is in private practice, Reno, NV.
Dr. Khanani explained that Tie2 is a transmembrane receptor expressed on vascular endothelial cells that exists in an activated state in normal healthy vasculature.
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In diabetic vasculature, Tie2 is deactivated, which leads to vascular destabilization and leakage. AKB-9778 acts by inhibiting VE-PTP, which is the most critical negative downregulator of Tie2.