Diabetes Drug TAX-875 Improves Glucose Control Without Increasing Hypoglycemia
Researchers say it is as effective as glimepiride with lower risk of drop in blood sugar - good news for about 11 million
seniors with type 2 diabetes
Feb. 27, 2012 - Only about half of those with type 2 diabetes most of them senior citizens - have their blood sugar levels on target,
but a new drug, studied by the University of Michigan shows promise in managing glucose levels. TAK-875 works by boosting the release of
insulin from pancreatic B cells, but only when diabetics need it most such as when glucose and fatty acids rise in the blood after a meal.
TAX-875, the researchers say, is as effective as glimepiride, but has a significantly lower risk of creating a dangerous
drop in blood sugar, called hypoglycemia.
Among the elderly in the U.S. those 65 years and older - 10.9 million, or 26.9 percent, had diabetes in 2010.
Type 2 diabetes is the most common form of diabetes accounting for 90 percent of the 150 million people in the United
States currently living with the disease. It is primarily caused by a lack of response to insulin which leads to high blood sugar and a
variety of chronic conditions.
The results of the phase 2 randomized trial were published Online First Sunday in The Lancet.
(Read more "About Diabetes" below news report.)
Free fatty acid receptor 1, also known as G protein-coupled receptor 40, or GPR40, plays a vital role in stimulating and
regulating the production of insulin.
It works by boosting the release of insulin from pancreatic β-cells when glucose and fatty acids rise in the blood, such
as after a meal, which results in a fall in blood glucose levels. Drugs that activate the FFAR1 receptor have the potential to help diabetics
release more insulin and improve control of blood glucose levels.
TAK-875 is a novel oral medication designed to enhance insulin secretion in a glucose-dependant manner, which means that
it has no effect on insulin secretion when glucose levels are normal, and as such has the potential to improve the control of blood sugar
levels without the risk of hypoglycemia.
In the study, Charles Burant, M.D., Ph.D., professor of internal medicine at the University of Michigan Health System,
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, a placebo, or glimepiride, a conventional diabetes treatment. The primary outcome was
change in hemogloblin A1c from the start of the study.
At 12 weeks, all doses of TAK-875 resulted in significant drops in HbA1c compared with 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 to 48 percent) reached the American Diabetics
Association target of HbA1c less than 7 percent within 12 weeks, compared with placebo (19 percent) and was similar to glimepiride (40
TAK-875 was generally well-tolerated. The incidence of hypoglycaemia was significantly lower for all doses of TAK-875
compared with glimepiride (2 percent compared to 19 percent), and was similar to placebo which was 2 percent.
The overall incidence of treatment-related side effects was similar for the TAK-875 groups and placebo groups (49
percent; all TAK-875 groups vs 48 percent), but higher in the glimepiride group (61 percent) because of the increased risk of hypoglycemia.
The authors say: In view of the frequent hypoglycaemia after treatment with sulfonylureas,the low-risk of hypoglycemia
after treatment with TAK-875 suggests that there may be therapeutic advantage of targeting FFAR1 in treating people with type 2 diabetes.
They conclude:We are truly excited about the potential of TAK-875 and are eager to conduct larger trials to find out how
well this drug works, how safe it is and what its place is in the treatment of diabetes.
TAK-875 significantly improved glycaemic control in patients with type 2 diabetes with minimum risk of hypoglycemia. The
results show that activation of FFAR1 is a viable therapeutic target for treatment of type 2 diabetes, authors say.
Note: Burant is an unpaid consultant and advisor to Takeda Global Research and Development which discovered TAK-875.
Diabetes means your blood glucose, or blood sugar, is too high. With Type 2
diabetes, the more common type, your body does not make or use insulin well. Insulin is a hormone that helps glucose get into your cells to
give them energy. Without insulin, too much glucose stays in your blood. Over time, high blood glucose can lead to
serious problems with your heart, eyes, kidneys, nerves, gums and teeth.
You have a higher risk of type 2 diabetes if you are older, obese, have a family history of diabetes, or do not exercise.
The symptoms of type 2 diabetes appear slowly. Some people do not notice symptoms at all. The symptoms can include
● Being very thirsty
● Urinating often
● Feeling very hungry or tired
● Losing weight without trying
● Having sores that heal slowly
● Having blurry eyesight
A blood test can show if you have diabetes. Many people can manage their diabetes through healthy eating, physical
activity, and blood glucose testing. Some people also need to take
Should I be tested for diabetes?
Anyone 45 years old or older should consider getting tested for diabetes. If you are 45 or older and overweight-see the
BMI chart -getting tested is strongly recommended. If you are younger than 45,
overweight, and have one or more of the
risk factors, you should consider getting tested. Ask your doctor for a fasting
blood glucose test or an oral glucose tolerance test. Your doctor will tell you if you have normal blood glucose, prediabetes, or diabetes.
● Among U.S. residents ages 65 years and older, 10.9 million, or 26.9 percent, had diabetes in 2010.
● Diabetes affects 25.8 million people of all ages - 8.3 percent of the U.S. population
● DIAGNOSED - 18.8 million people
● UNDIAGNOSED - 7.0 million people
● About 215,000 people younger than 20 years had diabetestype 1 or type 2in the United States in 2010.
● About 1.9 million people ages 20 years or older were newly diagnosed with diabetes in 2010 in the United States.
● In 20052008, based on fasting glucose or hemoglobin A1C (A1C) levels, 35 percent of U.S. adults ages 20 years or
older had prediabetes - 50 percent of adults ages 65 years or older. Applying this percentage to the entire U.S. population in 2010 yields an
estimated 79 million American adults ages 20 years or older with prediabetes.
● Diabetes is the leading cause of kidney failure, nontraumatic lower-limb amputations, and new cases of blindness
among adults in the United States.
● Diabetes is a major cause of heart disease and stroke.
● Diabetes is the seventh leading cause of death in the United States.
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