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New boost for drug candidates

pharmafile | December 5, 2012 | News story | Research and Development, Sales and Marketing Bayer, EFPIA, K4DD, Leiden 

A new project is trying to increase the hit rates of successful drug candidates by improving the way they are designed.

K4DD (Kinetics for Drug Discovery) is a five-year programme focusing on optimising binding kinetics, because a key factor in whether a drug will work in practice or not is the way in which the binding is coupled to its physiological target.

The Innovative Medicines Initiative, funded by the European Union and member companies of European pharma trade body EFPIA, is putting €20 million into the scheme.

The hope is that a greater understanding of kinetic aspects of the way drugs and their targets interact will help identify candidates in the early phases of drug discovery.

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Although many compounds perform well initially, there are a great number of failures – around 90% – in clinical studies due to lack of efficacy. Researchers believe that defining a drug candidate’s ‘kinotype’, as well as its affinity and selectivity, could be crucial for the future design of drugs. 

The 20-strong consortium of companies and organisations will also examine a novel approach to design, that of ‘target residence time’. This is the time a small molecule remains bound to its target protein – something that may be of greater importance for its effect in a patient than its affinity. 

Bayer HealthCare and Leiden University of the Netherlands will co-ordinate the work.

“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,” said Ad IJzerman, professor of medicinal chemistry at Leiden.

The arrangement goes far beyond a traditional one-on-one industry/academia tie-up, insists Anke Müller-Fahrnow, Bayer’s head of lead discovery in Berlin.

“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,” Müller-Fahrnow explained.

Adam Hill

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