Shares in Lexicon Pharmaceuticals (NASDAQ:LXRX) surged nearly 30% after the company reported results from a recently completed clinical trial for the solid dose formulation of its diabetes drug, LX4211. Previously studies have already been completed using a liquid dose formulation.
The clinical trial administered a single dose of two 150 mg tablets, six 50 mg tablets or a 300 mg liquid dose formulation in varying sequences at 5-day intervals over a total period of 15 days to 12 patients with type 2 diabetes.
Results from the study showed that administration of two 150 mg tablets “significantly increased” total GLP-1 (p=0.001), active GLP-1 (p=0.032) and PYY (p=0.004). All three are important mediators of glycemic and appetite control plus other metabolic parameters, the company noted.
“Notably, single doses of LX4211 produced rapid and significant improvement in post-prandial glucose (PPG) and fasting plasma glucose (FPG), consistent with results seen in the previous Phase 2 study.”
“Pharmacokinetic and pharmacodynamic data from the study indicated that the solid oral formulation worked as well as or better than the liquid formulation on key parameters of hormonal release, PPG and FPG.”
Lexicon now intends to move the solid dose formulation to a Phase 2b study in the second quarter of 2011.
LX4211 inhibits both sodium-glucose co-transporter type 1 and sodium-glucose co-transporter type 2, which are responsible for most of the glucose reabsorption performed by the kidney and gastrointestinal tract., respectively.
"The significant elevations of GLP-1 levels observed in the study are particularly important given its established relevance in the treatment of diabetes," said Brian Zambrowicz of Lexicon.
"Newly observed in this study was the effect of LX4211 on increasing circulating levels of PYY. We believe the rapid reduction in blood sugar levels after meals, the increase in GLP-1 and the increase in PYY are all associated with SGLT1 inhibition by LX4211 in the gastrointestinal tract."
PYY and GLP-1 are gastrointestinal-derived peptide hormones that have been associated with producing satiety and reducing food intake.