Aerpio’s Unique Approach to Activating Tie2

Joseph Gardner, president and CEO of Aerpio Therapeutics, acknowledged that his company is not alone in developing Tie2-activating agents to treat retinal disease, but at OIS@AAO 2016 he laid out the case for why his company’s programs should be taken seriously in the space.

Aerpio has two first-in-class products for treating retinopathies, both focused on activating the Tie2 pathway vital for stabilizing the retinal vasculature: AKB-9778, a novel small-molecule agent administered subcutaneously; and ARP-1536, a novel monoclonal antibody for intravitreal injection. The Phase II TIME-2 trial of AKB-9778 in diabetic retinopathy (DR) has been completed, while ARP-1536 should enter the clinic in the first quarter of 2018, Gardner said during the Posterior Segment Company Showcase.

Diving deeper into the TIME-2 trial, Gardner reported that AKB-9778 showed an ability to improve underlying DR in both eyes. TIME-2 involved three treatment arms: AKB-9778 alone, Lucentis (ranibizumab, Genentech) alone, and both agents in combination. In the study eye, 10% of patients in the AKB-9778-only arm and 11.4% in the combination arm showed more than a two-step improvement in DR severity score. However, because of the subcutaneous route of AKB-9778, 11.8% in the AKB-9778 arm showed a similar improvement in the fellow eye, an important fact as roughly 70% of patients have bilateral DR. “We’re gearing up to do a longer and larger study to validate this in a one-year nonproliferative diabetic retinopathy trial,” Gardner said.

Continuing, he explained that Aerpio’s other retinopathy product, ARP-1536, uses an alternative approach to target the vascular endothelial cell protein tyrosine phosphatase (VE-PTP), a downstream regulator of Tie2 that other agents in the pipeline are not addressing. “We think our approach is likely to be the most robust approach to activating Tie2 compared to Ang-2,” Gardner said. ARP-1536 has the potential to treat cystoid macular edema and wet age-related macular degeneration (AMD) and be used in coformulation with anti-VEGF agents. “We think this will be a very powerful next-generation drug for us that will go after the more traditional approaches of treating DME [diabetic macular edema] as well as wet AMD,” he said.

“Our approach to activating Tie2 is unique,” Gardner stated. “We have a portfolio that will give us proprietary products out to 2034, and we control all of the IP in our programs.”

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