By Matthew Willett

If there's a stork that brings validated targets from Millennium Pharmaceuticals Inc. to Bayer AG, its wings must be getting tired.

Since the pharmaceutical giant from Leverkusen, Germany, joined the genomics innovator from Cambridge, Mass., two years ago, a marriage that included a potential $465 million dowry, 70 bundles of joy have flown across the Atlantic.

And many of those little small-molecule wonders, Bayer said, show preclinical promise. Data on at least one target are likely to support the filing of an investigational new drug application by the end of this year.

Geoff Ginsburg, Millennium's senior program director, said it's a revolution in drug discovery, combining genomics and high-throughput screening to identify and validate drug targets at a rate of about 100 annually.

At that rate, he said, there is a possibility of overshooting the stated goal of 225 targets. That wouldn't hurt Millennium, which contracted to take back all but 31 of the targets from Bayer.

"It gives us an opportunity for more success in drug discovery," Ginsburg told BioWorld Today. "It's a great example of how an innovative approach to using the genome can put forward targets likely to be successful in a high-throughput fashion. We can apply genomic technology and high-throughput validation to the drug discovery process.

"The Millennium platform uses high-throughput genomics technology, bioinformatics, database generation and transcriptional profiling, to assign potential disease relevance to drug targets coming from the genome," he said. "We're moving rapidly then to high-throughput screening with Bayer, which develops chemistry emerging from the high-throughput screening and develops it into potential drug candidates."

Ginsburg said the method for drug discovery was designed two years ago to make maximum use of a sequenced genome. Then the company built its discovery program around the Bayer collaboration.

"What we had set out to do in the alliance with Bayer is lay the groundwork of how the Millennium internal drug discovery process would run," he said. "It's leveraged out of the platform, the database generation, the transcriptional profiling techniques and the tissue resources. It's all built on the upstream work done to enable the Bayer collaboration."

The companies entered the research alliance in 1998 and extended it in May 2000. Including a 14 percent equity investment in Millennium by Bayer over the five-year period, the deal was valued at $465 million. Millennium officials would not disclose the amount they've received to date. (See BioWorld Today, Sept. 24, 1998.)

"In general," Ginsburg said, "we're working with Bayer in several areas: oncology, hematology, cardiology, virology and pain in the central nervous system. It's a broad spectrum of disease entities."

He said the targets are traditional in nature: receptors, enzymes and ion channels.

Working with Bayer, he said, has made a difference in Millennium's internal drug discovery process. Combine that with being ahead of schedule and it's a happy two-year anniversary.

"Millennium has benefited from the challenge of this relationship, and has also learned a great deal from the collaboration with Bayer about drug discovery," Ginsburg said. "Bayer has learned a great deal about the value of genomics processes for drug discovery.

"I think this is a landmark type of relationship. It capitalizes on a great synergy of two powerful organizations - Millennium's prowess in genomics and Bayer's prowess in drug discovery and development. The two combined are really unsurpassed in the industry."