ABSTRACT

Despite the introduction of many new technologies such as high-throughput screening, combinatorial chemistry, and various -omics, the number of new drugs approved per year remains constant over several decades. At the same time, productivity, measured by number of drugs approved per year per billion dollars spent, ination adjusted, has trended down by more than a factor of 10 from 1950 to 2010 (Group 2011). Although multiple factors could cause this unwelcomed trend, overlooking important factors in early stage drug discovery, resulting in high attrition rates in different phases of clinical trials after substantial resources have already been spent, could be one contributor. Drug-binding kinetics could be one of these hidden factors.