MESA: measuring enzyme-substrate affinities

Today’s high drug-development failure rate—the primary cause of the high cost of new drugs—is driven by the industry’s inability to measure more than an infinitesimal number of drug-pro-tein interactions at one time. Now, MESA (mea-suring enzyme-substrate affinities) technology, developed at Los Alamos National Laboratory (LANL), makes it possible to measure a very large number of these interactions very quickly. The resulting early detection of toxicity will save hundreds of millions of dollars in drug develop-ment costs.MESA enables researchers to screen drugs for binding to proteins without the need for any fluorescent labels, which are as large as most drug molecules. Adding fluorescent labels leads to drugs with poor performance and many side effects. MESA images drug-protein binding us-ing the natural X-ray fluorescence intrinsic to unlabeled drug molecules.To commercialize the technology, Dr. Benja-min Warner, co-inventor of MESA, took an entrepreneurial leave of absence from LANL to found Caldera Pharmaceuticals, which acquired $7 million in private financing and licensed the MESA technology. Using MESA, Caldera is striving to save the $40-billion-a-year drug dis-covery industry billions of dollars by shortening the testing process and weeding out potentially dangerous drugs before they reach expensive clinical trials. To meet market demand, Caldera is currently developing a relatively inexpensive XRFlow machine that combines MESA with so-lution measurement for use by the pharmaceu-tical and biomedical research industry. Caldera has a working prototype of its new XRFlow de-vice and plans to introduce XRFlow to the mar-ket in early 2008. Caldera is also developing its own pharmaceutical pipeline by finding new uses for existing drugs.Every drug that successfully undergoes clinical trials costs $200 million or more in direct costs because so many trials fail. MESA will enable failure-prone drugs to be eliminated before costly animal and clinical trials begin. In addition, ad-verse drug reactions kill approximately 100,000 hospitalized patients annually and cause serious side effects in another 2.2 million people in the United States. MESA will enable physicians to prescribe the right drug from the start by screen-ing patients for their likely response to specific drugs.With the development of MESA, a 2005 R&D 100 Award winner for the lab, LANL has spun out a viable startup with a bright future based on its valuable contribution to the pharmaceutical industry.
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