Galectin Offers Results in Preclinical Model of GR-MD-02, Results Show Significant Disease Improvement

Galectin Therapeutics GALT, the leading developer of therapeutics that target galectin proteins to treat fibrosis and cancer, announced today that a preclinical study in a mouse model of NASH (non-alcoholic steatohepatitis, or fatty liver disease) demonstrated that oral administration of the Company's lead galectin-3 inhibitor, GR-MD-02, resulted in significant disease improvement. Diabetic mice, fed a high fat diet to induce NASH, were treated after the development of disease with either a vehicle control (n=8) or GR-MD-02 (n=9) administered orally five days out of seven for a total of four weeks. The liver weight, liver-to-body weight ratio, and plasma triglyceride levels were significantly reduced in the GR-MD-02 treated animals as compared to vehicle control animals (p<0.05). Blood indicators of liver damage, including plasma AST (aspartate aminotransferase), plasma ALT (alanine aminotransferase), and plasma total bilirubin (TB) also demonstrated a statistically significant reduction following oral treatment with GR-MD-02 and, in fact, levels were reduced back to near normal levels (see accompanying figure here). AST, ALT, and TB in normal animals (140 ± 86 U/L, 33 ± 8 U/L, 0.4 ± 0.0 mg/dL) were increased in the NASH animals treated with vehicle (293 ± 59 U/L, 87 ± 16 U/L, 0.56 ± 0.1 mg/dL) and were significantly reduced with oral GR-MD-02 treatment (159 ± 27 U/L, p<0.01; 46 ± 12 U/L, p<0.01; 0.4 ± 0.1 mg/dL, p<0.001). Each of these blood biomarkers indicate liver injury that improved with treatment. Finally, fibrosis of the liver was significantly reduced with treatment with GR-MD-02, as indicated by the liver hydroxyproline content, a biochemical marker of collagen in the liver. Liver hydroxyproline content in the normal liver (0.48 ± 0.07 µg/mg total protein) was increased in the NASH animals treated with vehicle (0.76 ± 0.14 µg/mg total protein) and was significantly reduced with oral GR-MD-02 treatment (0.56 ± 0.12 µg/mg total protein, p<0.01). "Oral activity of GR-MD-02 in this established preclinical model of NASH represents an important step in the development of galectin inhibitors and complements our ongoing clinical program of intravenous administration in patients with NASH with advanced fibrosis," said Dr. Peter G. Traber, President, Chief Executive Officer, and Chief Medical Officer of Galectin Therapeutics Inc. "We have evaluated various established technology platforms and are currently developing oral formulations with a contracted firm with the goal of developing an oral formulation for human studies as a follow on to our current clinical development program." The Company has an ongoing clinical trial of GR-MD-02 titled, "A Multi-Center, Partially Blinded, Maximum Tolerated Multiple Dose Escalation, Phase 1 Clinical Trial to Evaluate the Safety of GR-MD-02 in Subjects with Non-Alcoholic Steatohepatitis (NASH) with Advanced Hepatic Fibrosis." Trial design details can be found at http://clinicaltrials.gov/ct2/show/NCT01899859?term=gt-020&rank=1. In 2013, Galectin Therapeutics received Fast Track designation from the FDA for this clinical development program. FDA grants Fast Track designation to help expedite review and approval of drugs in development that treat serious or life threatening diseases and fill an unmet medical need.