BioWorld International Correspondent

BORNHEIM, Germany - Morphochem AG entered a research collaboration with Aventis Pharma AG that will use Morphochem's high-throughput evolutionary chemistry to develop proprietary compounds that interact with a novel, undisclosed target for the treatment of diabetes.

Separately, Morphochem will optimize a potential cancer drug with Tokyo-based Sosei Ltd. using its capabilities in multicomponent reaction chemistry.

Aventis Pharma, of Frankfurt, Germany, will fully fund the Munich-based Morphochem team working on the two-year project. Morphochem also will receive further payments on clinical milestones as well as royalties on marketed products, said Morphochem CEO Lutz Weber, who did not disclose further financial details.

"Evolutionary chemistry is comparable to evolution by mutations on the DNA level," Weber said. "Our code being subject to mutations in the computer is about components and parameters for reactions like solvents, temperature, reaction times."

Knowing how a small molecule should look and act to bind on a known target, Morphochem's software randomly modifies the parameters for synthesis of such a small molecule, Weber explained. "It's pure chance then which molecule is generated in such synthesis. It's very different from combinatorial chemistry, with just modifying side groups of given chemical backbones."

The Morphochem partner defines the target to develop a small molecule against. Morphochem synthesizes the molecules and puts them into its biological assays.

"If our molecules do a good job in the tests, synthesis of their successors is subject to further simulated mutations," Weber said. "In feasibility studies we already found effective optimized lead compounds for further drug development for Aventis during a half year's time," he said, adding that Morphochem does not synthesize thousands of variants to find an optimized lead, but gets by on less than a hundred variants, reducing screening processes significantly.

"We expect to see the first compounds in clinical research by 2002," Weber said.

The collaboration with Sosei relates to Sosei's lead telomerase inhibitor compound, which is associated with preventing the continuous cell division that characterizes malignant cancer. The compound will be optimized and developed using Morphochem's capabilities in multicomponent reaction chemistry (MCR), which is based on software that is able to produce diverse libraries of small, complex molecules similar to those found in nature.

"Our rapid optimization procedures using MCR chemistry techniques with Sosei's unique biological assays will accelerate the research and development of this promising lead candidate," Weber said.

Results from the collaboration, including intellectual property rights, will be shared equally between Sosei and Morphochem.

Morphochem was established as a university spinout in 1996. In its third financing round in July 2000 it raised EUR40.6 million. The company has 120 employees, working at Munich-based headquarters and at subsidiaries in Monmouth Junction/Princeton, N.J., and Basel, Switzerland.

No Comments