Diabetes is a major worldwide disease. The International Diabetes Foundation estimated that, in 2005, there were 194 million adults with diabetes worldwide, an increase of over 40% since 1995. Approximately 90% of diabetics, or 175 million people, suffer from type 2 diabetes, the adult-onset form of the disease. Type 2 diabetes is characterized by inadequate response to insulin and/or inadequate secretion of insulin as blood glucose levels rise. Although deaths due to cancer, stroke, and cardiovascular disease are declining, the death rates due to diabetes have increased by about 30% in the past 12 years, and life expectancy for persons with diabetes is approximately 15 years less than in those who do not have diabetes. Therapies for type 2 diabetes are directed toward correcting the body's inadequate response with oral and injectable medications, or directly modifying insulin levels by injection of insulin or insulin analogs. The worldwide market for diabetes medications exceeded $10 billion and oral anti-diabetes drugs exceeded $6 billion in 2004.

The Simbiosys diabetes discovery platform consists of assaying solutions for a portfolio of clinically validated as well as emerging therapeutic targets.

PTP1B Inhibitors

Several protein tyrosine phosphatases (PTPs), including PTPa, PTP-LAR, and PTP-1B, have been implicated as negative regulators of the insulin signaling pathway. PTP1B is involved in insulin and leptin signaling and is the primary mechanism for down-regulating both the insulin and leptin receptor signaling pathways. Studies have shown that animals deficient in PTP1B improve glucose regulation and lipid profiles, and resist weight gain when treated with a high fat diet. Evidences have helped validate PTP-1B as a potential therapeutic target in the treatment of diabetes type 2 and obesity. Several pharmaceutical companies are pursuing the development of PTP1B inhibitors with the most advanced candidates now entering phase I and II trials.

Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors

A novel mechanism for the treatment of type 2 diabetes is DPP-IV inhibitors. They decrease the breakdown of GLP-1 by extending the half-life of endogenous GLP-1. Investigational DPP-IV inhibitors offer an advantage over other novel therapies (e.g., GLP-1 agonists and amylin analogs) since they can be administered orally. There are various DPP-IV inhibitors in Phase I, II, and III trials. DPP-IV is a member of a family of serine peptidases that includes quiescent cell praline dipeptidases (QPP), DPP8, and DPP9. In studies, DPP-8/9 inhibitors produced alopecia, thrombocytopenia, reticulocytopenia, enlarged spleen, multiorgan histopathological changes, and even mortality. Therefore, the selectivity of clinical candidates to DPP-IV over DPP-8/9 is important to an optimal safety profile.


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