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news.Incyte Corporation has initiated a phase I clinical trial to evaluate the potential of INCB13739 as a new treatment for type 2 diabetes.
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INCB13739 is an orally available small molecule inhibitor of 11-beta hydroxysteroid dehydrogenase type 1 (11beta-HSD1), an enzyme that appears to be critical to the development of type 2 diabetes.
11beta-HSD1 converts inactive cortisone into the active glucocorticoid, cortisol, a natural antagonist of insulin action. Human clinical studies have long suggested an active role for cortisol in the pathogenesis of human type 2 diabetes, and recent data from preclinical studies have revealed that 11beta-HSD1 and local glucocorticoid production play a critical role in mediating the initiation of insulin resistance and progression to diabetes.
Selective inhibitors of 11beta-HSD1 may, therefore, provide a new class of drugs to treat type 2 diabetes, as well as conditions often associated with this disease, such as dyslipidemia, atherosclerosis, and coronary heart disease.
Current treatments for type 2 diabetes typically address individual components of the disease, and few therapies target the multiple risk factors that lead to the elevated cardiovascular risk associated with this condition. By selectively inhibiting 11beta-HSD1 and reducing the level of cortisol in key metabolic tissues, INCB13739 has the potential to provide a broad spectrum impact on the multiple components seen in patients with type 2 diabetes.
Incyte’s phase I trial is a double-blind, placebo-controlled, single and multiple dose-rising study designed to assess the safety and pharmacokinetics of INCB13739 in healthy volunteers.
The phase I program will also evaluate the ability of INCB13739 to inhibit 11beta-HSD1 activity in adipose tissue and liver of high body mass index (BMI) individuals. Preclinical studies have shown that 11beta-HSD1 activity in these two tissues may be a primary driver of insulin resistance and diabetes.
Provided the compound is safe, Incyte expects to initiate one-month phase IIa trials in type 2 diabetes patients later this year, which will allow the company to evaluate the effect of the compound on multiple disease parameters, including glucose production and insulin sensitivity.