Bayer and Leiden University coordinate consortium to optimise binding kinetics for drug candidates
Five-year study aims to improve drug design
Bayer HealthCare and Leiden University of The Netherlands will coordinate an international consortium, called Kinetics for Drug Discovery (K4DD) to optimise binding kinetics for drug candidates with the goal of improving drug design.
The K4DD consortium consists of pharma companies, universities, knowledge institutes and smaller companies from all over Europe. The 20 partners in the consortium are key European players in their fields.
Many drugs that seem successful in early phases of development fail in clinical studies due to lack of efficacy. There is mounting evidence that binding kinetics – the time a drug remains bound to its pharmaceutically relevant protein target – may be of greater importance for its effect in the patient than its binding affinity.
Binding kinetics is understood to be of high importance for eventual clinical drug efficacy. However, in spite of 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 fail, Bayer says.
Heptares will provide stabilised GPCRs (StaRs) to the consortium, as well as access to expertise and to its broader GPCR discovery platform, which makes the study of GPCR binding kinetics possible. In particular, Heptares' Biophysical Mapping technology has been designed and developed specifically to screen and study the binding kinetics of small molecules and antibody fragments in complex with StaRs, making it a powerful tool for GPCR lead discovery and optimisation.
Europe’s Innovative Medicines Initiative (IMI) is providing €20m to support the consortium.
Anke Müller-Fahrnow, vice president and head of lead discovery Berlin at Bayer HealthCare Global Drug Discovery, and coordinator of the K4DD consortium, said: ‘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.’
The five-year study of the drug-target interaction will start from the very first picoseconds to the eventual times of treatment.