Obesity is increasing at an alarming rate and the associated disorders, cancer, type 2 diabetes, fatty liver, hypertension, and atherosclerotic heart diseases are the leading causes of premature deaths in the developed world and a rapidly increasing problem in developing countries. Individuals who have the prevalent combination of increased central  adipose tissue, insulin resistance, low plasma HDL cholesterol and high plasma triglycerides exhibit an especially increased risk of developing cardiovascular complications.

Obesity-related disorders are a major challenge to health care systems worldwide. More than 170 million people are currently affected by type 2 diabetes. The disease is regarded to be epidemic in USA and is now with increasing incidence also affecting young people. Over 300 million people suffer from obesity and 1 billion have problems with being overweight. Cancer in many organs, for instance breast, colon, liver and prostate cancer, is also linked to obesity.

Small molecule AMPK activators

Cancer: Several tumor suppressors are part of the AMP pathway. AMPK act as negative regulator of the mammalian TOR (mTOR) pathway which is a key regulator of cell growth and proliferation and increasing evidence suggests that its deregulation is associated with human diseases, including cancer and diabetes. AMPK activators are therefore of great interest as anti-tumour drugs.

Diabetes: AMPK is a regulator of cellular and systemic energy homeostasis, and of lipid homeostasis. Today’s commonly used anti-diabetic drugs activate AMPK but only indirectly and with low efficacy. The BG800 small molecules are direct activators of AMPK.

The company´s BG800 compounds act as direct activators of AMPK. The compounds show potent in-vivo efficacy in animal models and are orally active. The BG800 project has generated optimized leads that serves as candidates for scale-up programs to enable selection of candidate drug suitable for further development.