Diabetes: 11ß-HSD-1 Program

Vitae Pharmaceuticals is rapidly advancing its 11ß-HSD-1 inhibitor program through the clinic in partnership with Boehringer Ingelheim for the treatment of diabetes and associated metabolic diseases.

11ß-HSD-1 is a recently validated, new diabetic target, which has broad, potential metabolic syndrome benefit.

• The diabetes market is forecast to reach $45 billion by 2016 up from $27 billion in 2009, or 9% CAGR.
• Overexpression of 11ß-HSD-1 in a preclinical, in vivo model leads to a metabolic syndrome-like phenotype, including increased obesity, hypertension, impaired glucose tolerance and hypertriglyceridemia.

Vitae Pharmaceuticals applied its drug discovery process to identify compounds that can inhibit 11ß-HSD-1 in both the liver and adipose tissue, a hurdle in the development of safe, bioavailable compounds.

• In a crowded IP space, Vitae Pharmaceuticals discovered multiple novel scaffolds within ~8 weeks.
• Lead optimization quickly produced attractive compounds with picomolar potency, excellent selectivity and safety and PK/PD consistent with once-daily dosing.
• Based on the preclinical findings, as well as clinical evidence showing inhibition of 11ß-HSD-1 reduces both glucose and lipids in diabetic patients, 11ß-HSD-1 represents a highly attractive therapeutic target.

Under a 2007 collaboration with Boehringer Ingelheim, Vitae Pharmaceuticals has received $37 million in upfront and research funding with the potential to earn up to $300 million in milestones.

• Vitae Pharmaceuticals earned a $14 million milestone payment in 2010 for the start of Phase 1 clinical trials.  To date Vitae Pharmaceuticals has earned $26 million in milestone payments.