Islet Sciences, Inc. Highlights Remogliflozin Etabonate as Novel Treatment for Non-alcoholic Steatohepatitis (NASH)

Company Presents Positive Preclinical Efficacy Results at ICE/ENDO 2014 Meeting

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Jun 23, 2014, 08:00 ET

RALEIGH, N.C., June 23, 2014 /PRNewswire/ -- Islet Sciences, Inc. (OTCQB: ISLT), a biopharmaceutical company developing new medicines and technologies for the treatment and diagnosis of metabolic disease, recently presented a peer-reviewed poster highlighting the unique properties of its selective sodium glucose transporter 2 (SGLT2) inhibitor, remogliflozin etabonate (a prodrug of active remogliflozin), as a novel treatment for non-alcoholic steatohepatitis (NASH) and its precursor, non-alcoholic fatty liver disease (NAFLD). The poster was presented this past Saturday at ICE/ENDO 2014, the joint meeting of the International Society of Endocrinology and the Endocrine Society, at the McCormick Place West in Chicago, IL, June 21-24.

Remogliflozin etabonate is uniquely positioned as an effective therapy for NAFLD/NASH due to its proven insulin-sensitizing activity as a selective SGLT2 inhibitor, combined with its intrinsic anti-oxidant activity, which is independent of its ability to inhibit SGLT2 and may be differentiated from other drugs in this class.

Arun Sanyal, M.D., Professor of Medicine at Virginia Commonwealth University Medical Center and former President of the American Association for the Study of Liver Diseases (AASLD) commented, "The combination of two distinct mechanisms of action – improved insulin sensitivity via selective SGLT2 inhibition and inherent antioxidant activity – into a single, small molecule, oral drug may be significant for the future treatment of NAFLD/NASH, which is becoming an even greater public health issue as the global incidence of obesity and diabetes continue to rise."

In its peer-reviewed poster titled, "Remogliflozin Etabonate Improves Non-Alcoholic Steatohepatitis," Islet Sciences described positive preclinical efficacy results for remogliflozin etabonate in a diet-induced model of fatty liver disease. In this study, diet-induced obese (DIO) mice treated orally with remogliflozin etabonate displayed reduced liver transaminases (AST and ALT; 35% and 80%, respectively), which are well-recognized biomarkers for NAFLD/NASH, compared to paired-fed controls over the four-week treatment period. Islet also observed a reduction in liver transaminases in its 12-week Phase 2b study of remogliflozin etabonate in diabetic patients. Treatment of DIO mice with remogliflozin etabonate also resulted in significantly reduced liver weight (50%) as well as total liver TAG content (40%), compared to paired-fed controls. In another study performed with genetically obese (KKA^y) mice, an approximately 50% decrease in liver triglycerides was observed after 8 weeks of oral remogliflozin etabonate treatment. Remogliflozin etabonate also demonstrated robust in vivo anti-oxidant activity, reducing the level of oxidative stress markers, both in plasma and in the liver (30%), compared to controls. This appears to be a unique property of active remogliflozin, which also demonstrated greater than ten times the antioxidant activity of canagliflozin and dapagliflozin when measured by oxygen radical antioxidant capacity in vitro.

William Wilkison, Ph.D., Islet Sciences' Chief Operating Officer, stated, "The preclinical results presented at ENDO, combined with what we have observed in the clinic, establishes a strong rationale for pursuing fatty liver disease as a potential indication for remogliflozin etabonate. Its ability to reduce glucose levels and increase insulin sensitivity in diabetic patients, which we've demonstrated in our previous clinical studies, combined with the significant reductions in liver steatosis and enzyme levels we've described in this preclinical study are highly encouraging. Importantly, we are pleased to see remogliflozin's positive effect on reducing the oxidative stress that occurs with fatty liver disease, which may be mediated by remogliflozin's innate anti-oxidant activity. This is a unique and potentially meaningful differentiator for our best-in-class SGLT2 inhibitor."

NAFLD affects up to 25% of the U.S. population, and may reach as high as 50% by 2030¹. Early stage NAFLD is marked by increased fat in the liver stored as triacylglycerol (TAG), which is often caused by obesity and/or insulin resistance. It is hypothesized that fatty liver (hepatic steatosis), combined with changes in lipid metabolism, create a highly lipotoxic environment characterized by an increase in oxidative cellular stress and resultant decrease in liver function. If not treated, NAFLD can progress to more severe NASH, which can cause significant scarring of the liver and development of cirrhosis and other serious complications. There are no therapies approved specifically for treating NAFLD/NASH, although anti-diabetic medications and anti-oxidants are being examined based on these important hallmarks of the disease.

BHV Pharma owns exclusive rights to remogliflozin etabonate in the global territory outside of Japan, Korea and Taiwan, through a license from Kissei Pharmaceuticals.

About Islet Sciences
Islet Sciences, Inc., a biopharmaceutical company based in Raleigh, NC, is developing new medicines and technologies for the treatment and diagnosis of metabolic disease. On March 13, 2014, the Company announced the execution of a binding letter of intent to acquire BHV Pharma. The combined pipeline includes remogliflozin etabonate for the treatment of type II diabetes and NASH, a cell-based transplantation therapy for insulin-dependent diabetes; first-in-class immune-modulating small molecule IL-12 inhibitors targeting beta-cell preservation, and a PCR-based molecular diagnostic measuring beta-cell loss for the diagnosis of type 1 diabetes or onset of insulin dependent type 2 diabetes. For more information, please visit http://www.isletsciences.com.

About Kissei Pharmaceutical
Kissei Pharmaceutical Co., Ltd. was founded in 1946 and has grown into one of Japan's leading pharmaceutical companies. Kissei's management vision is to be an R&D-oriented pharmaceutical company that contributes to the health of people around the world through developing and commercializing innovative drugs. Kissei is actively pursuing collaborations with many companies to strengthen its R&D pipeline, and also promoting global expansion by licensing out original agents as an important management strategy. Kissei ranks metabolism & endocrinology as one of its major R&D areas and is putting significant effort into the development of novel therapeutic agents. For more information on Kissei, please see the international website http://www.kissei.co.jp/.

¹Ford ES, Giles WH, Dietz WH. Prevalence of the metabolic syndrome among US adults: findings from the third National Health and Nutrition Examination Survey. JAMA. 2002; 287(3):356-9.

Forward-Looking Statements
This press release contains forward-looking statements. Forward-looking statements for Islet Sciences, Inc. reflect current expectations, as of the date of this press release, and involve certain risks and uncertainties. Actual results could differ materially from those anticipated in these forward- looking statements as a result of various factors. Factors that could cause future results to materially differ from the recent results or those projected in forward-looking statements include the risks described in the Islet Science, Inc.'s reports filed with the Securities and Exchange Commission. The Company's further development is highly dependent on future medical and research developments and market acceptance, which is outside of the Company's control.

Contacts:
Tiberend Strategic Advisors, Inc.

Joshua Drumm, Ph.D. (Investors)
[email protected]; (212) 375-2664

Amy Wheeler (Media)
[email protected]; (646) 362-5750

Islet Sciences, Inc.
[email protected]; (919) 480-1518

SOURCE Islet Sciences, Inc.