Drug development at Aerpio.

Tie2 Activators

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AKB-9778 Summary

Healthy cells that line blood vessels are essential for human well being. Compromises to the integrity of the vasculature can lead to blood proteins and other components leaking into the tissues, a condition known as vascular (or capillary) leak syndrome. Vascular leak can be localized to a single tissue (as in retinopathy and macular edema), or it can be systemic leading to life-threatening consequences such as cerebral and pulmonary edema, hypotension and shock.

Vascular stabilization may provide extraordinary benefits in a wide variety of diseases, including diabetes (particularly diabetic vascular complications), oncology, and systemic vascular leak syndromes such as sepsis. In addition, vascular stabilization may reduce vascular leak associated with a number of cancer treatments.

AKB-9778 is a small molecule, Tie2 activating agent that effectively blocks vascular leak and pathologic angiogenesis in multiple disease conditions. It is being developed for the treatment of diabetic retinopathy.

How AKB-9778 Works

Tie2 signaling is responsible for stabilizing blood vessels and maintaining vascular integrity. The VE-PTP enzyme (vascular endothelial protein tyrosine phosphatase), the target of AKB-9778, acts as a negative regulator, or brake, at the Tie2 receptor. AKB-9778 works by inhibiting VE-PTP and effectively removes this negative regulation on the Tie2 receptor. This action restores Tie2 signaling and vascular integrity.

Indication for AKB-9778

In collaboration with investigators world-wide, Aerpio has demonstrated the efficacy of AKB-9778 in a wide range of animal models of human disease. The efficacy in vascular diseases of the eye has been particularly impressive. Therefore, Aerpio will initially develop AKB-9778 for the treatment of diabetic retinopathy as there remains considerable unmet medical need.

Publications about AKB-9778

Enhanced Benefit in Diabetic Macular Edema from AKB-9778 Tie2 Activation Combined with Vascular Endothelial Growth Factor Suppression.

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Targeting VE-PTP Activates Tie2 and Stabilizes the Ocular Vasculature

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Treatment of Diabetic Macular Edema with an Inhibitor of Vascular Endothelial-Protein Tyrosine Phosphatase That Activates Tie2

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