An innovative approach targeting the Tie2 pathway: Subcutaneous AKB-9778 for the treatment of non-proliferative diabetic retinopathy (NPDR)

AKB-9778 is a small molecule inhibitor of VE-PTP, the most critical negative regulator of Tie2 in diseased blood vessels. It binds to and inhibits the intracellular catalytic domain of VE-PTP that inactivates Tie2. Inhibition of VE-PTP has shown the ability to activate the Tie2 receptor irrespective of extracellular levels of its binding ligands, angiopoietin-1 (agonist) or angiopoietin-2 (antagonist), and may represent the most efficient pharmacologic approach to restoring Tie2 activation.

Subcutaneous Treatment Affects both Eyes in Diabetic Retinopathy

AKB-9778 is patient self-administered via a subcutaneous injection, similar to insulin. Pharmacokinetic studies have shown that AKB-9778 is quickly taken into circulation and rapidly reaches the target tissue, the retinal vasculature. In TIME-2, a Phase 2a, proof-of-concept study, AKB-9778 monotherapy, showed the ability to improve underlying diabetic retinopathy by 2 or more steps on the ETDRS diabetic retinopathy severity scale in both eyes. Based on these results, Aerpio has initiated a Phase 2b study, TIME-2b, studying AKB-9778 administered once or twice daily versus placebo in patients with NPDR.

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