Aerpio Initiates Phase 1b Clinical Trial of Topical Ocular Formulation of AKB-9778 for Primary Open Angle Glaucoma

CINCINNATI–(BUSINESS WIRE)–Aerpio Pharmaceuticals, Inc. (Nasdaq: ARPO), a biopharmaceutical company
focused on developing compounds that activate Tie2 to treat ocular
diseases and diabetic complications, today announced dosing of the first
subject in a Phase 1b trial of a topical ocular formulation of AKB-9778
in development for treatment of primary open angle glaucoma (POAG).

The Phase 1 study is a double-masked, multiple-ascending dose trial and
will enroll four cohorts of 12 subjects. Subjects will receive
increasing daily doses of a topical ocular formulation of AKB-9778 or
placebo for seven days. The primary endpoint of the trial is ocular
safety and tolerability, with IOP lowering as the key pharmacodynamic
endpoint.

“POAG is characterized by increased IOP leading to optic nerve and
neuroretina anomalies and progressive visual field defects,” said Kevin
Peters, M.D., Chief Scientific Officer of Aerpio Pharmaceuticals.
“Reducing IOP has proven to be the only clinical approach shown to slow
or prevent vision loss. The conventional outflow pathway, consisting of
the trabecular meshwork and a specialized vessel called Schlemm’s canal,
controls IOP and has been identified as the site of increased resistance
to aqueous humor outflow in POAG. We have recently shown in animal
models that topical ocular dosing of AKB-9778 lowers IOP via its action
on Schlemm’s canal, and in two sequential Phase 2 clinical studies, we
have shown that subcutaneous administration of AKB-9778 significantly
reduced IOP in ocular normotensive patients. Bases on these data, we
believe that AKB-9778 could provide a novel and differentiated approach
to treating POAG and the first approach that directly affects Schlemm’s
canal. We look forward to sharing the results of this study by the end
of 2019.”

About AKB-9778

AKB-9778 binds to and inhibits vascular endothelial protein tyrosine
phosphatase (VE-PTP), an important negative regulator of Tie2. Decreased
Tie2 activity contributes to vascular instability in many diseases
including diabetes. AKB-9778 activates the Tie2 receptor irrespective of
extracellular levels of its binding ligands, angiopoietin-1 (agonist) or
angiopoietin-2 (antagonist) and may be the most efficient pharmacologic
approach to maintain normal Tie2 activation.

About Aerpio Pharmaceuticals

Aerpio Pharmaceuticals, Inc. is a biopharmaceutical company focused on
advancing first-in-class compounds that activate Tie2 to treat ocular
diseases and complications of diabetes. Tie2 is an important regulator
of vascular stability and its down-regulation is found in patients with
diabetes and other conditions. Down-regulation is caused by activation
of two inhibitors of Tie2, VE-PTP and Ang-2. The Company’s lead
compound, AKB-9778, is being investigated, in a topical drop
formulation, for its potential as a treatment for open-angle glaucoma.
For more information, please visit www.aerpio.com

Contacts

Investor & Media:
Aerpio
Pharmaceuticals, Inc.
Michael Rogers
Chief Financial
Officer
mrogers@aerpio.com

or

Burns McClellan, on behalf of Aerpio Pharmaceuticals, Inc.
Media:
Nancie
Steinberg / Robert Flamm, Ph.D.
nsteinberg@burnsmc.com
/ rflamm@burnsmc.com
or
Investors:
John
Grimaldi
jgrimaldi@burnsmc.com