The process of creating a new drug is lengthy and complex. From discovery to development to market, there are numerous pitfalls. In this report, Kalorama focuses on one of the trickiest yet also most promising areas: the interface between discovery and development known as lead optimization.
The pressure is on: get better lead compounds faster and at less cost. The amount of money wasted on leads that fail is excessive. And the attrition rate to get a lead is huge. One estimate is that for every 100,000 compounds screened, about 100 hits are identified. Of these 100 hits, only one makes it to the lead compound stage. Between 40% and 60% of these lead compounds fail ADMET testing. Only 10% of IND submissions get approved. Over 72% of the costs for drug development are wasted on failures.
Three years ago, industry experts were saying that something radically different needs to happen, that the whole drug discovery process needs to be re-engineered. Today, the solutions are beginning to emerge: new assays, new computer models, better libraries, and high-throughput screening for ADMET characteristics. Early ADMET is now in the development stage, and improvements are coming rapidly from many directions. Researchers are now getting the tools to assess ADMET earlier in the discovery process.
The market for these tools and for lead optimization services is growing rapidly. This fact, in addition to overwhelming interest in the lead optimization areas of Kalorama Information’s May 2003 report Outsourcing in Drug Discovery, caused us to take a deeper look at this exciting area of research.