Bayer HealthCare and Leiden University of The Netherlands will coordinate a newly founded international consortium, dubbed "K4DD" (Kinetics for Drug Discovery), which has been launched to explore a novel concept in modern drug discovery and to tackle a big problem in the development of new drugs. Although successful in early phases of development, many drug candidates fail in clinical studies due to lack of efficacy. The new five-year project will focus on 'optimizing binding kinetics' for drug candidates with the goal of improving drug design. The consortium is financially supported with 20 million Euro by Europe's Innovative Medicines Initiative (IMI).
There is a clear understanding today that compound binding characteristics to its molecular target (binding kinetics) is of high importance for eventual clinical drug efficacy. Therefore, drug discovery has also focused on the optimization of these drug-target interactions, mostly with respect to affinity and selectivity. However, despite the efforts in finding high-affinity and selective compounds, attrition rates of candidate drugs are still disappointingly high and almost 90% of clinical drug candidates that enter clinical trials still fail.
Dr. Anke Müller-Fahrnow, Vice President and Head of Lead Discovery Berlin at Bayer HealthCare Global Drug Discovery, and Coordinator of the K4DD consortium, comments: "K4DD is an excellent example of a project in which public-private partnerships enable a collaborative research approach to tackle specific drug discovery problems of today and to come up with novel concepts in modern drug discovery. We have assembled a large experienced team of kinetics experts from academic institutions and industrial partners to create a Europe-wide network of complementary capabilities extending far beyond the scope of a traditional ‘one-on-one’ industry-academia collaboration."
The new concept of 'target residence time', the subject of the IMI consortium "K4DD", represents a novel approach in early drug discovery with the final goal of optimizing drug design. 'Residence time' is the time a low-molecular weight (small) molecule remains bound to its target protein and it may be of greater importance for its effect in a patient than its affinity. The consortium was launched to optimize the binding kinetics of each possible drug candidate in the future, i.e. define its 'kinotype', next to its affinity and selectivity.
Prof. Ad P. IJzerman, professor of medicinal chemistry at the Leiden/Amsterdam Center for Drug Research of Leiden University, The Netherlands, and the academic lead of the K4DD consortium, is enthusiastic: "We welcome the unique opportunity afforded by this IMI initiative. The broad support from Europe's pharma companies and the European Union combined with the expertise within our institute and our partners will enable us to achieve the leverage necessary to tackle this complex project. The joint efforts of this consortium will generate a critical mass to employ drug-target interaction data as a basis for improved drug candidate design and hopefully better patient therapy."
The K4DD consortium consists of pharma companies, universities, knowledge institutes and smaller companies from all over Europe. The 20 partners in the consortium are European key players in their fields: they have been and are involved in the structure elucidation of drug targets, are at the forefront of bioanalytical techniques, are world-leaders in pharmacology, and bring the best of computational resources for heavy computer calculations. This ensemble of technologies allows the study of the drug-target interaction from the very first picoseconds to the eventual times of treatment (often days and more). The goal of this project is that kinetic aspects of drug-target interactions can routinely be studied in robust and accessible assays for all main drug target classes within and outside the consortium. 'Kinotypic' knowledge should guide the identification and optimization process of drug candidates in the early phases of drug discovery in the future.
About the Innovative Medicines Initiative (IMI)
IMI is the world's largest public-private partnership in health. IMI is improving the environment for pharmaceutical innovation in Europe by engaging and supporting networks of industrial and academic experts in collaborative research projects. The European Union contributes €1 billion to the IMI research program, which is matched by in kind contributions worth at least another €1 billion from the member companies of the European Federation of Pharmaceutical Industries and Associations (EFPIA). The Innovative Medicines Initiative is currently funding 37 projects, many of which are already producing impressive results. The projects all address major bottlenecks which will accelerate the development of safer and more effective treatments for patients. The research leading to these results has received support from the Innovative Medicines Initiative Joint Undertaking under grant agreement n° 115366, resources of which are composed of financial contribution from the European Union's Seventh Framework Program (FP7/2007-2013) and EFPIA companies' in kind contribution.
About Bayer HealthCare
The Bayer Group is a global enterprise with core competencies in the fields of health care, agriculture and high-tech materials. Bayer HealthCare, a subgroup of Bayer AG with annual sales of EUR 17.2 billion (2011), is one of the world’s leading, innovative companies in the healthcare and medical products industry and is based in Leverkusen, Germany. The company combines the global activities of the Animal Health, Consumer Care, Medical Care and Pharmaceuticals divisions. Bayer HealthCare's aim is to discover, develop, manufacture and market products that will improve human and animal health worldwide. Bayer HealthCare has a global workforce of 55,700 employees (Dec 31, 2011) and is represented in more than 100 countries.