Diabetes R & D Pipeline: 11beta-HSD1 Inhibitors-Aarkstore Enterprise

April 8, 2010 - PRLog -- 11beta-HSD1 (11beta-hydroxysteroid dehydrogenase type 1) antagonists are insulin sensitizers. 11beta-HSD1 is an enzyme that converts inactive cortisone into potent, biologically active hormone, cortisol. This conversion occurs within cells of key metabolic tissues including liver, adipose tissue, muscle tissue, and pancreas. Cortisol elevates blood glucose levels by increasing glucose production in liver, and by inhibiting uptake and disposal of glucose in muscle and adipose tissues. Consequently, 11beta-HSD1 mediated production of cortisol contributes to insulin resistance, development of type 2 diabetes, and associated cardiovascular diseases

Preclinical studies have demonstrated that transgenic mice overexpressing 11beta-HSD1-selectively in adipose tissue develop type 2 diabetes and visceral obesity, in comparison to 11beta-HSD1 knockout mouse, which displays normoglycemia and normal weight.

11beta-HSD1 inhibitors were found to increase insulin sensitivity and glucose tolerance and to have anti-obesity effects. In addition,  atherosclerotic plaques in apoE knockout mice were improved after treatment with 11beta- HSD1 inhibitors.

11beta-HSD1 inhibitors appear to be attractive research and development products for the treatment of type 2 diabetes because a large number of major biotechnology and pharmaceutical companies are involved in their development, and this pipeline, although very young, already has 70% of products in clinical stage of development.


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