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PMT13, a novel PPARgamma agonist for the treatment of diabetes and obesity In both the US and the UK the incidence of obesity is increasing by about 1% per year, a tendency related to the rise in other serious co-morbidities. As a general guide, obesity increases the likelihood of death from coronary heart disease by 25%. In addition, obese individuals are at twice the risk of developing diabetes. Many people are obese, suffer cardiovascular problems and are also diabetic, leading to the hypothesis that the coexistence of these diseases is not a coincidence, but that a common underlying abnormality allows them to develop. In 1988 it was suggested that co-morbid obesity and diabetes was related to insulin resistance, and hence the insulin resistance syndrome was first described. It is estimated that this syndrome affects 70 to 80 million Americans and is characterized by a failure of insulin to stimulate glucose utilization and uptake into tissues. Total development activity relating to type 2 diabetes treatments has increased dramatically since 1998 and now accounts for 2% of all therapeutic candidates or marketed products. This is largely due to the ascendancy of insulin sensitizers. Although attention is being paid to the development of novel strategies for increasing insulin sensitivity (see our recent report on Glycogen synthase kinase inhibitors for one novel approach). PPAR agonists continue to lead this field with the two lead insulin sensitizers, Actos (Pioglitazone) and Avandia (Rosiglitazone) capturing the lion's share of the market for anti-diabetic agents. Even so, insulin sensitizers that have not yet reached the market are likely to generate considerable sales upon launch. Dr Reddys' PMT13 is one such molecule showing similar PPARgamma activation as rosiglitazone, without any activity against PPARalpha or PPARdelta. Consequently, PMT13 was found to be a molecule with antidiabetic, hypolipidaemic and insulin-sensitizing properties. Additionally, PMT13 inhibited liver glucose-6-phosphatase activity and increased lipoprotein lipase activity. The compound also showed a good safety margin. Therefore, PMT13 can be a potential drug candidate for future development. Entry date October, 2002 Adapted from Chakrabarti et al, Diabetes Obes Metab 2002 Sep;4(5):319-28
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