Apr 23, 2014

Chromatin closes series E financing Aerpio Therapeutics, Inc. , a clinical-stage biopharmaceutical company focused on advancing innovative therapies for vascular diseases, today announced that it closed a $22M financing round led by new investor OrbiMed, with existing investors Novartis Venture Funds, Satter Investment Management, Kearny Venture Partners, Venture Investors, Triathlon Medical Ventures and Athenian Venture Partners. Proceeds will support expanded development of AKB-9778, a small molecule activator of Tie2, currently in a Phase 2 trial for the treatment of diabetic macular edema (DME), and the advancement of AKB-4924, a small-molecule HIF1 activator, into clinical development for inflammatory bowel disease (IBD). Chau Q. Khuong, Private Equity Partner at OrbiMed, will join Aerpio’s Board of Directors. "Aerpio's unique approach to activating Tie2 with AKB-9778 has demonstrated safety and efficacy in early clinical trials and holds great promise for treatment of DME and other retinal diseases, as well as unmet needs outside of ophthalmology,” said Mr. Khuong. “OrbiMed is pleased to support the expanded development of AKB-9778, as well as the Company’s promising HIF1 activator program. " "OrbiMed has an impressive track record of supporting both public and private companies as they bring innovative new medicines to market, and we are excited to have them join our investor syndicate," stated Joseph Gardner, PhD, President and CEO of Aerpio. Aerpio recently initiated a randomized, double-masked, double dummy, Phase 2 study designed to assess the safety and efficacy of AKB-9778 administered over three months as monotherapy and as an adjunct with ranibizumab in subjects with DME. The primary endpoints of the study are change from baseline in visual acuity and change from baseline in central retinal thickness. Additionally, Aerpio is prioritizing further therapeutic opportunities for AKB-9778 and expects to initiate development in a second target indication before year end. With this financing, Aerpio will also progress a second pipeline candidate, AKB-4924, and activator of HIF1, into clinical development. HIF1 is critical for the regulation of innate immune responses and maintenance of epithelial barrier function, particularly in the gut and skin. HIF1 activators represent a promising new class of drugs with potential for potent and specific modulation of innate immunity. AKB-4924 has demonstrated robust activity in preclinical models of ulcerative colitis and Crohn's disease. About AKB-9778 AKB‐9778 is a first-in-class small molecule that works by inhibiting the human protein tyrosine phosphatase β (HPTPβ) enzyme, which acts as a negative regulator of the Tie2 receptor. By inhibiting this negative regulator, Tie2 signaling is restored, overcoming the effects of the Ang2‐induced vascular destabilization. Aerpio is currently focusing development of its lead candidate, AKB‐9778, in diabetic macular edema (DME), however, Tie2 activators have potential utility in a range of important clinical indications. In a Phase 1b/2a study in DME patients, AKB-9778 was well tolerated throughout 28 days of dosing, with evidence of disease improvement in some patients. A Phase 2 study to confirm efficacy of AKB-9778 alone and in combination with ranibizumab in patients with DME is currently ongoing. About Aerpio Therapeutics Aerpio Therapeutics, Inc. is a clinical‐stage biopharmaceutical company focused on advancing innovative therapies for vascular diseases. Aerpio is a leader in the development of small molecule drugs based on Tie2 activation and the stabilization of hypoxia-inducible factor 1α (HIF‐1α). The Company’s lead program, AKB‐9778, is a first‐in‐class stabilizer of the Tie2 pathway and is in clinical development for diabetic macular edema. More information is available at www.aerpio.com . About OrbiMed OrbiMed is a leading investment firm dedicated exclusively to the healthcare sector with approximately $10 billion in assets under management. OrbiMed invests globally across the spectrum of healthcare companies on a worldwide basis, from venture capital start-ups to large multinational companies. OrbiMed's team includes over 60 experienced professionals with offices in New York, San Francisco, Shanghai, Mumbai and Herzliya. OrbiMed manages a series of private equity funds, public equity funds, royalty and debt funds, and other investment vehicles. Aerpio Therapeutics, Inc.