FDA approves linagliptin for oral treatment of type 2 diabetes

BY BIOCAT

Pharmaceutical companies Boehringer Ingelheim Pharmaceuticals —with their Spanish headquarters in Sant Cugat del Vallès (Barcelona)— and Eli Lilly & Co have announced the American health authorities’ (FDA) approval of linagliptin, a prescription drug that, in combination with diet and exercise, reduces blood glucose levels in patients with type 2 diabetes.

This is the first treatment of its type to be approved in a concentrated dose (5 mg taken once a day) and can be taken with or without food. Linagliptin reduces blood sugar levels by increasing incretin levels, thus achieving increased insulin levels not only after meals but throughout the day.

FDA approval of linagliptin is significant because it will allow all patients to take one dose per day, regardless of their renal or hepatic deterioration.

Clearance of linagliptin at a 5 mg daily dose was based on data from a clinical trial program including some 4,000 adults with type 2 diabetes. Three placebo-controlled studies evaluated linagliptin either as monotherapy or in combination with the drugs most commonly prescribed for type 2 diabetes: metformin, sulphonylurea and pioglitazone. The studies confirmed linagliptin significantly reduced glycosated hemoglobin (HbA1c), which is the index used in clinical practice to monitor blood glucose levels, by up to 0.7% when used as monotherapy. When used in combination with metformin, sulphonylurea and sulphonylurea with metformin, adding linagliptin resulted in a significant reduction of A1c levels (0.6%, 0.5% and 0.6% respectively). The initial combination of linagliptin and pioglitazone also showed a significant decrease in A1c levels (0.5%).

Linagliptin treatment also significantly reduced fasting plasma glucose levels compared to placebo treatment when used in combination with metformin, sulphonylurea, or pioglitazone.  Linagliptin treatment produced a significant decrease in postprandial glucose levels (two hours after meals) compared to placebos as monotherapy and in combination with metformin.

FDA approval of linagliptina is the first milestone under the framework of the international alliance established by Boehringer Ingelheim and Eli Lilly & Co to fight diabetes in January 2011.

Next step, EU and Japan

This drug is currently being reviewed by health authorities in the European Union and Japan.

Most of Boehringer Ingelheim’s net sales still come from the United States. In 2010, these sales generated more than €5,700 million, which is 46% of their net sales. Although this is still down 8.6% from 2009, as the result of a special situation that led one of their patents to expire in the US, the business is showing positive development.
In Europe and the area of Asia, Australasia and Africa (AAA), Boehringer Ingelheim increased their sales. The AAA Region proved to be a dynamic market, with net sales increasing 11.6%. Markets in developing countries and in the Asia Pacific region are of strategic importance for this pharmaceutical company, although precautions have been taken for 2011 due to recent events in Japan.