RALEIGH, N.C., April 16, 2014 (GLOBE NEWSWIRE) -- Islet Sciences, Inc. (OTCQB:ISLT) and BHV Pharma today announced positive results from two 12-week phase 2b clinical studies of remogliflozin etabonate in type 2 diabetics. The primary end point was HbA1c with secondary end points of fasting plasma glucose, serum lipids, body weight, safety and tolerability. Remogliflozin etabonate is a selective SGLT2 inhibitor indicated for type 2 diabetes and NASH. Islet Sciences will present the full results of the two phase 2b clinical studies at the 74th American Diabetes Association Scientific Sessions in San Francisco, June 13-17th.
Both phase 2b studies were multicenter, randomized, double-blind, placebo-controlled, pioglitazone-controlled, parallel-group, dose-ranging studies evaluating the efficacy, safety, and tolerability of multiple remogliflozin etabonate doses for 12 weeks in treatment-naïve subjects with type 2 diabetes. One study dosed remogliflozin etabonate once-daily and the other dosed remogliflozin etabonate twice-daily over the twelve week study period.
At Week 12, twice-daily dosing of remogliflozin etabonate produced a statistically significant trend in dose response for change from baseline (p<0.001) with changes in HbA1c ranging from -1.0% to -1.4%. Once-daily dosing demonstrated a trend in dose response for change from baseline in HbA1c above the lowest dose (p < 0.047) with changes in HbA1c ranging from -0.5% to -0.8%. Decreases from baseline for FPG were statistically and significantly different from placebo in all treatment groups. A statistically significant decrease in body weight (1.36 to 3.51 kg) from baseline was seen in all twice-daily remogliflozin etabonate treatment groups by Week 12 versus placebo and a statistically significant decrease in body weight versus placebo (1.44 to 1.51 kg) from baseline was seen in all once-daily remogliflozin etabonate groups above the lowest dose. In general, remogliflozin etabonate was efficacious and well tolerated with either dose regimen.
The primary differentiating factor between dosing regimens was duration of drug plasma exposure relative to evening post prandial glucose excursions and subject's sleep period. While twice-daily dosing provided greater relative reductions in HbA1c and body weight, we also observed increases in LDL-c and incidence rates of genital fungal infections similar to what has been demonstrated with other SGLT2 inhibitors. Once-daily dosing of remogliflozin etabonate demonstrated lower reductions in HbA1c and body weight relative to twice-daily dosing but generally resulted in no change in LDL-c and lower incidence rates of genital fungal infections compared to placebo. These results are consistent with the longer plasma exposure from twice-daily dosing having a greater effect on evening postprandial glucose excursions and shorter plasma exposure from once-daily dosing limiting the undesirable effects of nighttime inhibition of SGLT2. As a result, BHV and Islet Sciences have developed a novel once-daily bi-phasic formulation of remogliflozin etabonate that is expected to maintain the efficacy of twice-daily dosing and the improved safety and tolerability profile demonstrated with once-daily dosing.
"The results of these two studies are very positive in their own right, but what's exciting is the additional formulation work we have done as a result of what we've learned from these data," said Islet COO, Dr. William Wilkison. "Based on our phase 2b results, we have learned more about the biology of the mechanism and have developed a once-daily formulation that will maximize the effect on post-prandial glucose and therefore efficacy, while reducing side-effects commonly associated with inhibition of SGLT2. And at the same time, with a selective SGLT2 inhibitor we avoid the potential side effects of the more broadly expressed SGLT1 gene which appears to play a role in glucose modulation in cardiac tissue."
About Islet Sciences, Inc.
Islet Sciences, Inc., a biopharmaceutical company based in Raleigh, NC, is developing new medicines and technologies for the diagnosis and treatment 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 SGLT2 Inhibitors and Remogliflozin Etabonate
SGLT2 inhibitors block reabsorption of glucose in the kidney resulting in reduced blood sugar and A1c levels. They are the only oral anti-diabetics that provide significant HbA1c lowering with clinically relevant weight loss through an insulin-independent, beta-cell sparing mechanism of action.
Remogliflozin etabonate is a selective SGLT2 inhibitor in phase 2 clinical development for type 2 diabetes and NASH. Remogliflozin has been dosed in over 800 subjects in more than 20 clinical trials.
About BHV Pharma
BHV Pharma is a privately held pharmaceutical company based in Research Triangle Park, North Carolina. The company is focused on developing therapeutics for the treatment of metabolic diseases. http://www.bhvpharma.com.
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 are outside the Company's control.