FDA approves linagliptin tablets for the treatment of type 2 diabetes

Boehringer Ingelheim and Eli Lilly and Company announced that the U.S. Food and Drug Administration (FDA) has approved linagliptin tablets, a prescription medication used along with diet and exercise to lower blood sugar in adults with type 2 diabetes. 1 The FDA has approved linagliptin as a monotherapy or in combination with other commonly prescribed medications for type 2 diabetes—such as metformin, sulphonylurea and pioglitazone — to reduce haemoglobin A1c (HbA1c or A1c) levels by a mean of up to -0.7 percent (compared to placebo). 2 HbA1c is measured in people with diabetes to provide an index of blood sugar control for the previous two to three months. It is used as a marker of efficacy of antihyperglycaemic therapies.

Linagliptin belongs to a class of prescription medications called dipeptidyl peptidase-4 (DPP-4) inhibitors and is the first member of its class to be approved at one dosage strength (5 mg, once daily). 1 With linagliptin, no dose adjustment is recommended for patients with kidney or liver impairment. Linagliptin is a tablet that can be taken with or without food. Linagliptin lowers blood sugar in a glucose-dependent manner by increasing incretin levels (GLP-1), which increase insulin levels after meals and throughout the day. 1

“Many people with type 2 diabetes are not able to control their blood sugar with diet and exercise alone and may also require one or more medications,” said John Gerich M.D., Professor of Medicine, University of Rochester School of Medicine. “The FDA approval of linagliptin is exciting because there is only one dose to remember for all patients, regardless of kidney or liver impairment. With linagliptin, physicians will have another option for managing type 2 diabetes, a potentially devastating condition.”

Linagliptin 5mg once daily was approved based on a clinical trial programme which included approximately 4,000 adults with type 2 diabetes. Included in the programme were three placebo-controlled studies evaluating linagliptin as monotherapy and in combination with the commonly prescribed oral antihyperglycaemic medications metformin and suphonylurea. Linagliptin showed statistically significant mean difference in HbA1c from placebo of up to -0.7 2 percent when used as monotherapy In patients who were not adequately controlled on metformin or metformin plus sulphonylurea, the addition of linagliptin resulted in a statistically significant mean difference in HbA1c from placebo of -0.6 percent. 3-4

In a fourth study, the initial combination of linagliptin and pioglitazone was compared with pioglitazone alone. 5 The difference in the adjusted mean HbA1c between the linagliptin and placebo groups was -0.5% (p<0.0001). 5 For patients taking linagliptin plus pioglitazone, mean HbA1c change from baseline was -1.1 percent compared to a change of -0.6 percent for patients taking pioglitazone alone (p < 0.0001). 5

Treatment with linagliptin also produced significant reductions in fasting plasma glucose (FPG) compared to placebo, when used as monotherapy and in combination with metformin, sulfonylurea and/or pioglitazone. 2-3, 5-6 Treatment with linagliptin produced significant reductions in two-hour post-prandial glucose (PPG) levels compared with placebo as monotherapy 2 and when used in combination with metformin. 3 FPG is used to determine glucose levels in a fasting state (usually upon wakening in the morning), and PPG is used to determine glucose levels after meals (usually two hours after eating).