Elcelyx Therapeutics to Present Metformin DR Data at American Diabetes Association 75th Scientific Sessions

Studies Confirm Glucose Lowering with Gut-Restricted Metformin and no Increased Plasma Lactate with Delivery to the IIeum

SAN DIEGO, June 6, 2015 – Elcelyx Therapeutics announced today that the Company will present two posters related to its Metformin DR program at the American Diabetes Association 75th Scientific Sessions in Boston, MA. The data outlined in these posters support further development of Metformin DR, a novel delayed-release formulation of metformin that targets delivery to the lower bowel. Delivery to the lower bowel results in reduced absorption into the plasma and markedly reduced exposure while maintaining the glucose-lowering effect. As such, Metformin DR is being developed as a potential therapy to serve renally impaired type 2 diabetes patients who are currently contraindicated for metformin therapy since Metformin DR would not be expected to increase the risk of lactic acidosis in this patient population.

Mark Fineman, Ph.D., Senior Vice President of Research & Development at Elcelyx will present an analysis of the Company’s Phase 2b study along with the findings of a separate study that confirmed the equivalent efficacy of Metformin DR dosed once-daily vs twice daily. The Phase 2b clinical trial was a multicenter, double-blind dose-finding study evaluating Metformin DR once-daily doses of 1000, 800 and 600 milligrams compared to placebo and demonstrated the glucose lowering effects of a gut- restricted metformin formulation. The primary endpoint of the study was fasting plasma glucose at four weeks of treatment. The median reductions in fasting glucose from baseline (~160 mg/dL) at 4 weeks ranged from 11 to 18 mg/dL across the Metformin DR doses tested compared to a reduction of 4 mg/dL for placebo. Two comparator arms with generic extended-release metformin dosed once-daily at 1000 and 2000 milligrams were included in the study to assess the relative potency of gut-restricted metformin compared to currently available metformin. Reductions with Metformin XR doses ranged from 12 to 25 mg/dL suggesting an increase in apparent potency of Metformin DR vs Metformin XR of approximately 40%. The median fasting plasma metformin concentrations with Metformin DR were ~20% that of equivalent doses of Metformin XR. Plasma lactate concentrations were also lower with Metformin DR than with Metformin XR.

The Company will present a second poster describing studies showing that intragastric and intravenous delivery of metformin resulted in increased plasma lactate levels in rat models, whereas intra-ileum administration did not. In addition, blood lactate concentrations were highly correlated to plasma metformin concentrations. Targeted delivery to the Ileum was not associated with an increase in blood lactate levels even at very high doses. The results of this preclinical study supports the clinical findings and further suggest that patients with renal impairment taking effective doses of Metformin DR (targeted to the ileum) would not have increased accumulation of metformin in the circulation, a condition that could predispose patients to lactic acidosis.

“Metformin is the preferred first-line and foundational agent to treat type 2 diabetes but nearly 4 million patients in the U.S. are contraindicated to this therapy due to concomitant renal impairment” said Dr. Ralph DeFronzo, Professor of Medicine and Chief of the Diabetes Division at the University of Texas Health Science Center and the Audie L. Murphy Memorial Veterans Administration Hospital in San Antonio, Texas. “Together, these Metformin DR results hold the promise of providing a once-daily, equally efficacious metformin alternative to the renally impaired type 2 diabetes patients, a population that is currently underserved by existing oral therapies.” Dr. DeFronzo was an advisor on the Phase 2b Metformin DR clinical study.

Elcelyx Therapeutics’ Posters at ADA:

Title: The Primary Glucose Lowering Effect of Metformin Resides in the Gut Not the Circulation— Results from 7‐Day and 12‐Week Studies

  • Date and Time: Sunday, June 7, Noon to 2:00 p.m.
  • Poster 1207P, Category: 01E Clinical Therapeutics/New Technology–Oral Agents

Hyperlink to abstract

Title: Metformin Administration into the Ileum Is Not Associated with Increased Systemic Lactate

  • Date and Time: Saturday, June 6, 11:30 a.m. to 1:30 p.m.
  • Poster 1313P, Category: 01F Clinical Therapeutics/New Technology–Pharmacologic Treatment of Complications

Hyperlink to abstract

About Elcelyx Therapeutics Inc.
Elcelyx was founded in 2010 to advance Gut Sensory Modulation (GSM) technology based on the elucidation that enteroendocrine cells, including the L-cell located in the lining of the lower gut, can be modulated locally to elicit systemic physiological and pharmacological effects.  This discovery affords a potentially safety-advantaged platform to develop novel therapies as well as re-position existing therapies to meet serious unmet needs. Elcelyx is based in San Diego, CA. For more information, visit www.elcelyx.com.

Media Contact:
Elcelyx Therapeutics Inc.
Joanne Leonard
Chief Financial Officer
joanne.leonard@elcelyx.com
(858) 876-1814 ext.112

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