Background:

LGD-6972 is a glucagon receptor antagonist.

LGD-6972 has linear plasma pharmacokinetics consistent with once daily dosing that is comparable in healthy and T2DM subjects. Dose-dependent decreases in fasting plasma glucose are observed in all groups with a maximum of 3.15 mM (56.8 mg/dL) on day 14 in T2DM subjects. LGD-6972 also reduces plasma glucose in the postprandial state. Dose-dependent increases in fasting plasma glucagon are observed, but glucagon levels decrease and insulin levels increase after an oral glucose load in T2DM subjects. LGD-6972 is well tolerated at the doses tested without dose-related or clinically meaningful changes in clinical laboratory parameters. No subject experiences hypoglycaemia[1].

[1]. Vajda EG, et al. Pharmacokinetics and pharmacodynamics of single and multiple doses of the glucagon receptor antagonist LGD-6972 in healthy subjects and subjects with type 2 diabetes mellitus. Diabetes Obes Metab. 2017 Jan;19(1):24-32.