Vitae Pharmaceuticals Receives $14 Million Milestone Payment as Boehringer Ingelheim Advances Lead Compound into Phase I Clinical Trials

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Tue Jun 29, 2010 7:30am EDT

Program Targets 11beta-HSD-1 for the Treatment of Diabetes and Other Metabolic
Syndrome Disorders
FORT WASHINGTON, Pa.--(Business Wire)--
Vitae Pharmaceuticals, Inc., an integrated discovery and development company,
today announced that it has earned a $14 million clinical milestone payment from
Boehringer Ingelheim, one of the world`s 20 leading pharmaceutical companies.
Vitae`s 11beta-hydroxysteroid dehydrogenase (HSD)-1 is targeted for the
treatment of diabetes and metabolic syndrome-related diseases in a strategic
alliance with Boehringer Ingelheim. The payment recognizes Boehringer
Ingelheim`s recent advancement of a small molecule inhibitor of 11beta-HSD-1
into Phase I clinical trials. 

"Inhibition of 11beta-HSD-1 represents an important new mechanism of action for
treating diabetic patients," commented Dr. Richard Gregg, Vitae`s Chief
Scientific Officer. "This program addresses several features of the metabolic
syndrome, a combination of disorders, including abdominal obesity, high blood
pressure and insulin resistance or glucose intolerance, all of which contribute
to an increased risk of coronary heart disease, stroke and Type 2 diabetes." Dr.
Gregg continued, "Boehringer Ingelheim and Vitae have worked well together on
this program. We are very pleased with the quality of the lead candidate and
look forward to further building its profile as it advances in the clinic." 

Vitae and Boehringer Ingelheim initiated their strategic 11beta-HSD-1 alliance
in October of 2007. Under the terms of that agreement, the companies combined
their respective research programs, working together to identify and advance
novel 11beta-HSD-1 inhibitors. Vitae has now achieved three performance
milestones totaling $26 million of a potential $300 million under the
collaboration. Vitae is also eligible to receive royalty payments from
Boehringer Ingelheim on sales of products commercialized under the
collaboration. 

About 11beta-HSD-1 Inhibition

11beta-HSD-1 is an enzyme that converts the biologically inactive steroid
cortisone into the active hormone cortisol. Cortisol is known to cause
resistance to the action of insulin in multiple target tissues, including liver,
muscle and adipose tissue. Overexpression of 11beta-HSD-1 in mouse adipose
tissue leads to a metabolic syndrome-like phenotype, including increased central
obesity, hypertension, impaired glucose tolerance and hypertriglyceridemia. In
contrast, 11beta-HSD-1 knockout (KO) mice resist visceral obesity and diabetes
through improved function of insulin in liver and adipose tissues, consistent
with the beneficial effects of enzyme inhibition. Early clinical evidence has
shown that inhibiting 11beta-HSD-1 can reduce glucose and lipids in diabetic
patients. These data indicate that elevated levels of adipose and liver
11beta-HSD-1 are detrimental to metabolic control. Pharmacological inhibition of
11beta-HSD-1 represents an attractive therapeutic target for diabetes and
treating cardiovascular risk factors associated with the metabolic syndrome. 

About Diabetes

Nearly 30 million adults suffer from Type 2 diabetes in the United States; 194
million worldwide. These numbers are expected to nearly double in the next
twenty years. In the U.S., one in four Americans suffer from obesity/diabetes;
in addition, over 40 million people in the U.S. are diagnosed in the
pre-diabetic state. An aging population, sedentary lifestyle and rapidly growing
incidence of obesity are all contributing to the dramatic rise in prevalence of
diabetes. The current U.S. diabetic drug market exceeds $10 billion, and is
predicted to grow to $45 billion by 2020. 

Vitae Pharmaceuticals

Vitae Pharmaceuticals is a development-stage biopharmaceutical company building
a portfolio of novel, small molecule, best-in-class compounds that address large
markets, including chronic kidney disease, diabetes and Alzheimer`s disease.
Vitae`s lead compound, VTP-27999, is a wholly owned, novel, potent and selective
renin inhibitor offering the potential for superior renal protection in patients
suffering from chronic kidney disease. The compound is advancing through Phase I
clinical trials; the Company expects to be in Phase II by the end of 2010. 

Vitae is an expert in structure-based drug discovery and combines a proprietary
technical platform with the experience and insight of world class scientists to
advance best-in-class compounds for high value, hard-to-drug targets. Vitae`s
proprietary, discovery platform has clear advantages in creating and analyzing
novel drug candidates that meet pre-defined physicochemical characteristics. The
accuracy and speed of this system has enabled Vitae to solve challenging targets
in multiple therapeutic areas -- discovering and advancing attractive compounds
in a rapid and highly capital efficient manner. Vitae Pharmaceuticals is
financed by leading corporate and venture capital investors; its last venture
round was in 2004. Vitae`s 45 scientists are located in Fort Washington,
Pennsylvania. For additional information, please visit the Company`s website,
www.vitaepharma.com.

Burns McClellan on behalf of Vitae
Justin Jackson, Michelle Szwarcberg (media), 212-213-0006
jjackson@burnsmc.commszwarcberg@burnsmc.com

Copyright Business Wire 2010

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