Rosiglitazone (Molecule of the Month for September 2006)
Diabetes, Avandia, Avandamet, Avandaryl
Rosiglitazone is a thiazolidinedione drug that is currently used to treat diabetes. It works by helping the body respond to its own insulin and may also preserve the ability to make insulin. It is being marketed as Avandia® by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet®). Another combination drug approved by the FDA is Avandaryl® (with glimepiride).
A study involving 5,269 participants at 191 clinics in 21 countries showed that taking the drug rosiglitazone reduced the chance of getting type 2 diabetes by 60 per cent among those at high risk. The trial was co-ordinated by the Diabetes Trials Unit at Oxford University and the Canadian Cardiovascular Collaboration at McMaster University, Canada. The results have major implications for future health care. The study included 5,269 people worldwide whose average age was 55 and whose glucose level was starting to rise, putting them at high risk of diabetes, but who did not have the condition. Participants took rosiglitazone (a thiazolidinedione), ramipril (an angiotensin-converting enzyme inhibitor), or a placebo over a period of three years. Among study participants taking rosiglitazone, only 12 per cent developed diabetes, compared to 26 percent who were taking the placebo. Rosiglitazone also normalized glucose levels in 51 percent of participants versus 30 percent of those taking a placebo. It benefited all participants, and particularly those who weighed the most.
Type 2 diabetes develops when the body can no longer produce sufficient insulin to meet demand, often in people where insulin already works less well than normal (known as insulin resistance). Rising glucose levels, as seen in all the participants of the trial, are a warning sign. Type 2 diabetes is the more common of the two main types and accounts for 85–95 per cent of all people with diabetes. It is strongly associated with being overweight. More than five percent of all adults have a diagnosis of type 2 diabetes, and this rate is rising rapidly throughout the world, due in part to the increase in weight and reduction in physical activity in both developed and developing countries. Those with type 2 diabetes require lifelong therapy to reduce their high risk of further complications such as blindness, kidney failure, amputations, heart attacks, strokes and premature death.
Formal Chemical Name (IUPAC)
Update by Karl Harrison
(Molecule of the Month for September 2006 )