Bayer and Millennium announce genome-derived oncology drug candidate selected for first human studies

Synergistic alliance accelerates drug discovery

11-Jan-2001

Bayer and Millennium Pharmaceuticals, Inc. today announced their joint success in employing a new research paradigm resulting in the rapid discovery of the first genome-derived small molecule drug candidate to emerge from the companies' joint research alliance. This novel compound is believed to be the first small molecule drug candidate discovered against a genomics-derived target. Initiation of phase I human clinical trials for this drug candidate are expected to begin as soon as feasible in 2001.

In less than 18 months Bayer and Millennium were able to move from gene discovery to clinical candidate status. This streamlined "targets by class" approach began with the profiling of novel genes in various tumor models from which a novel gene and protein was discovered and linked to cancer using Millennium's high-throughput gene discovery platform. Bayer developed screening assays against the new target and screened its vast chemical library against the new protein using proprietary ultra high-throughput methods. Thus, a new chemical compound was discovered that was further optimized through tumor-specific in vitro and in vivo studies to proceed to clinical candidate status (a chemical compound that has a metabolism and toxicity profile suitable for human studies). This rapid and shared discovery program validates the innovative genomics-based approach to drug discovery and ultimately could accelerate the development of breakthrough therapies.

This success is indicative of the synergies forged between the Millenniumand Bayer alliance. By integrating large-scale genetics, genomics, automation and informatics, Millennium searched for disease-relevant targets that were promising for drug discovery. Bayer brought its leading high tech drug discovery platform to the project including the breadth and strength of chemistry and pharmacology expertise.

"The value that we may be able to extract from the genome is phenomenal," said Mark Levin, chairman and chief executive officer of Millennium. "The accelerated discovery of this compound is an excellent example of the power of Millennium's technology platform combined with the synergistic strengths of our alliance with Bayer to discover therapies that can revolutionize medicine and drug discovery."

"Bayer long ago recognized the incredible potential for use of genomic-based drug discovery," said Professor Wolfgang Hartwig, executive vicepresident of pharmaceuticals research at Bayer. "This is a major milestone for the pharmaceutical industry as well as for the relationship between Bayer and Millennium, confirming the value of Bayer's strategy of using leading-edge genomic technologies for drug discovery. We look forward to the continued success of the alliance."

Alliance Background

The primary goal of the alliance, which began in September 1998, is for Millennium to supply 225 important new drug targets in seven different indications relevant for cardiovascular diseases, cancer, pain, hematology and viral infections. From those identified by the alliance, Bayer will select drug targets for its exclusive use and the remainder will be available to Millennium to use in its proprietary drug development efforts. Millennium has delivered to Bayer more than 80 disease-relevant validated drug targets in the first two years of their five-year research alliance.

In return for total payments of up to $465 million over a five-year period, including an equity investment in Millennium, Bayer receives access to key technologies in modern genome research and a flow of new genomics-based targets for drug development.

Drug targets are proteins expressed by human genes that can be used to discover and develop small molecule drugs. All of the drugs produced by the pharmaceutical industry during the last 100 years of research are based on approximately 500 drug targets. Th

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