Ligand Pharmaceuticals Incorporated ( LGND) announces results from a Phase 1b clinical trial with LGD-6972 that demonstrate favorable safety, tolerability and pharmacokinetics in normal healthy volunteers and in subjects with type 2 diabetes mellitus. The trial results also demonstrate a robust, dose-dependent reduction of fasting plasma glucose. LGD-6972 is Ligand’s novel glucagon receptor antagonist, and these results were presented at the American Diabetes Association’s 75thScientific Sessions meeting underway in Boston.
Glucagon receptor antagonists are the leading non-insulin mechanism in development for the treatment of type 2 diabetes. Based on earlier data and these latest results, Ligand believes LGD-6972 has best-in-class properties given its potency, preliminary effectiveness in lowering plasma glucose in patients with type 2 diabetes and its safety profile demonstrated in two Ligand-sponsored clinical trials.
In this randomized, double-blind, placebo-controlled trial, LGD-6972 was administered in sequential increasing oral doses daily over two weeks to both healthy subjects and subjects with type 2 diabetes. A total of 48 subjects were enrolled in the trial.
Highlights of the study include:
LGD-6972 tested at 5mg, 10mg and 15mg was safe and well-tolerated with no clinically significant or dose-dependent changes in hematology, clinical chemistry or urinalysis panels, ECG or vital signs. There were no serious adverse events and no study discontinuations. All treatment-emergent adverse events were of mild or moderate severity (grade 1 or 2).Plasma levels increased linearly with LGD-6972 dosage, and the pharmacokinetic profiles were comparable between normal and type 2 diabetes subjects, supporting once-daily dosing.LGD-6972 lowered fasting plasma glucose in normal subjects and in subjects with type 2 diabetes. Glucose was reduced throughout the 14-day dosing period. Baseline adjusted glucose values showed dose-dependent effects of LGD-6972 in type 2 diabetic subjects with a maximal decrease of 60 mg/dL.7 point glucose measurements were performed at baseline and Day 14 and illustrated that LGD-6972 decreased glucose throughout a 24-hour period in both fasting and post-prandial states.LGD-6972 is a highly potent and selective glucagon receptor antagonist and is a promising agent for the treatment of type 2 diabetes.Ligand is preparing to initiate a Phase 2 trial with LGD-6972 in 2016 with the goal to establish additional safety and efficacy for the program in 12 consecutive weeks of dosing in subjects with type 2 diabetes. Approximately 100 subjects will be enrolled in this randomized, double-blind, multicenter trial. The trial is estimated to cost approximately $10 million and should be completed in 2017. Any incremental increase to Ligand’s annual R&D spending as a result of this program is expected to be covered within Ligand’s financial operations, and there is no change to the company’s long-term earnings guidance... |
