Treating type 2 diabetes patients using Boehringer Ingelheim’s (BI) oral candidate, linagliptin, leads to statistically significant and sustained reductions in blood sugar levels, according to data from four Phase III trials. The international placebo-controlled studies showed that when used as monotherapy or in combination with either metformin, pioglitazone, or metformin plus a sulfonylurea, treatment using linagliptin led to significant reductions in blood levels of hemoglobin A1c (HbA1c), fasting plasma glucose and postprandial glucose. The Phase III trial data was presented at the recent American Diabetes Association Scientific Sessions in Orlando.
Treatment using the once-daily oral drug candidate also led to improvements in beta cell function, the decline in which is believed to represent a key factor in the progression of type 2 diabetes, BI states. Additional data from the trials showed that in patients with mild and moderate renal impairment, linagliptin blood plasma levels were comparable to those in type 2 diabetes patients with normal renal function. BI says this finding is consistent with data suggesting linagliptin may have a primarily nonrenal route of excretion.
Linagliptin is a once-daily oral dipeptidyl peptidase-4 inhibitor designed to target the incretin hormones GLP-1 and GIP. The drug candidate is the most advanced in BI’s diabetes pipeline. The global clinical program for linagliptin includes studies of up to two years and trials in type 2 diabetes patients with renal impairment. The firm is separately developing a sodium-glucose cotransporter inhibitor candidate BI-10773, which is designed to block tubular reabsorption of glucose in the kidney. BI says Phase II trials with BI-10773 have now been concluded.
More upstream in the firm’s diabetes pipeline is an 11β-HSD1 inhibitor, which is believed to work by lowering intracellular cortisol concentrations and helping to prevent cortisol-related detriments in terms of insulin sensitivity, blood lipid levels, and vascular function.