Boehringer hopes cash injection will turbocharge diabetes and obesity programme

The pharma heavyweight will pay its small rival $36.5m (€25.8m) upfront and up to $300m in milestone payments in order to combine their drug discovery programmes aimed at finding compounds that block 11 beta-hydroxysteroid dehydrogenase Type 1 (11-beta-HSD-1). Further payments may be achieved with additional compounds and/or indications. This enzyme is involved in cortisol production, which in turn blocks insulin activity in multiple tissues, and is therefore being examined by a number of companies as a potential target to develop treatments for diabetes and metabolic disorders, such as obesity and hypertension. "Vitae has discovered and rapidly advanced novel, highly potent 11beta-HSD1 inhibitors in multiple series over the past 20 months using its unique structure-based drug design technology Contour,"​ said Jeffrey Hatfield, CEO of Vitae. At a time when drug discovery costs are spiralling ever higher, the ability to speed up the process and therefore save money is appealing to every company, and it is undoubtedly this ability which attracted Boehringer to Vitae. Not only that, but with rival companies already having 11-beta-HSD-1 in Phase I and Phase II trials (Amgen and Incyte respectively), Boehringer could do with a helping hand if it is not to be left behind. In return, Vitae gets access to the resources and capabilities of a much bigger company and the two together are hoping to get their drugs into the clinic faster. Contour is a structure-based drug design platform that can design and optimise compounds within the binding site of a target protein and simultaneously predict their binding activity. The technology uses machine learning to increase speed and accuracy and Vitae claims it can generate "tens of thousands of drug-like compounds per day while simultaneously predicting their three-dimensional structure and binding affinities." ​​The algorithm's accuracy can then be tested by comparing predicted structural conformation with known x-ray co-crystal structures and validated by a comparison of predicted activity with biological data. Given 194 million adults worldwide suffer from Type II diabetes, new drug targets in thsi field could potentially provide a breakthrough in treatment. This need for new treatment strategies is ever greater since the number of those numbers are expected to nearly double in the next twenty years, thanks to an aging population, sedentary lifestyle and rapidly growing incidence of obesity (over 90 per cent of obese people have Type II diabetes). Not only that, but the current US market for these drugs exceeds $10bn, and is predicted to grow to $45bn by 2020. Over-expression of 11beta-HSD-1 in murine adipose tissue leads to increased central obesity, hypertension, impaired glucose tolerance, and hypertriglyceridaemia. In contrast, 11beta-HSD1 knockout mice resist visceral obesity and diabetes through improved liver and adipose tissue function. Early clinical evidence has shown that inhibiting 11-beta-HSD1 can reduce glucose and lipids in diabetic patients, indicating elevated adipose or liver 11-beta-HSD-1 is detrimental for metabolic control. As part of the deal, Boehringer will lead development and commercialisation of products but Vitae will have the right to develop products independently for certain indications.