Drugs like TAK-875 activate FFA1, which plays a vital role in insulin production and regulation. The insulin monomer (top) is biologically active, while the insulin hexamer (bottom), is the stored form.

Under Control

An effective new diabetes drug also reduces incidence of hypoglycemia

issue 16 | summer 2012

Emerging research shows that TAK-875, a new drug for Type 2 diabetes, improves glycemic control and is equally effective as glimepiride but has a significantly lower risk of hypoglycemia. Drugs like TAK-875 that activate the free fatty acid receptor (FFA1) have the potential to help diabetics release more insulin and improve control of blood glucose levels with few side effects.

"In view of the frequent hypoglycemia after treatment with sulfonylureas, the low-risk of hypoglycemia after treatment with TAK-875 suggests that there may be a therapeutic advantage to targeting FFA1 in treating people with Type 2 diabetes," says researcher Charles Burant, M.D., Ph.D., professor of Internal Medicine and the Robert C. and Veronica Atkins Professor of Metabolism at the U-M Medical School.

Free fatty acid receptor 1 plays a vital role in stimulating and regulating the production of insulin. It works by boosting the release of insulin from pancreatic beta cells when glucose and fatty acids rise in the blood, such as after a meal, which results in a fall in blood glucose levels. TAK-875 is a novel oral medication designed to enhance insulin secretion in a glucose-dependent manner, which means that it has no effect on insulin secretion when glucose levels are normal.

In a study published in Lancet, Burant and colleagues randomly assigned 426 patients with Type 2 diabetes who were not achieving adequate glucose control through diet, exercise or metformin treatment to one of five doses of TAK-875, placebo or glimepiride. The primary outcome was change in glycosylated hemoglobin (HbA1c) from the start of the study.

At 12 weeks, all doses of TAK-875 resulted in significant drops in HbA1c compared with a placebo. A similar reduction occurred in patients given glimepiride. At a TAK-875 dose of 25 mg or higher, about twice as many patients (33 percent to 48 percent) reached the American Diabetes Association target HbA1c of less than 7 percent within 12 weeks, compared with a placebo (19 percent), and was similar to glyburide (40 percent).

TAK-875 was generally well-tolerated. The incidence of hypoglycemia was significantly lower for all doses of TAK-875 compared with glim-e-pir-ide (2 percent versus 19 percent) and was similar to a placebo (2 percent).

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