BioWorld International Correspondent

LONDON - Cresset BiMolecular Discovery Ltd. is looking for funding and/or a partner to help it move up from a platform technology and services company, and develop an in-house drug portfolio.

"What we are looking for is step change," Beatrice Leigh, CEO, told BioWorld International. "We have proven technology, now we need to move it up the value chain."

The company's FieldScreen drug discovery software is based on analyzing the molecular fields on the surface of a target, rather than its molecular structure. Structurally different drug molecules can bind to the same region of a protein and have the same therapeutic effect, if they have similar molecular fields.

Cresset has used its software to determine the molecular fields of 1.5 million commercially available compounds. These can be matched against the molecular fields or FieldPrint, of an existing lead to find compounds with similar activity but diverse structures.

The technology makes it possible to substitute peptides with non-peptides, and steroids with non-steroids. While it can be used for any target, it offers a way of applying in silico drug discovery disciplines to targets for which there are no crystal structures, or for those such G protein-coupled receptors (GPCR) that are hard to crystallize.

To date the technology has been applied to more than 30 projects on a fee-for-service basis. Cresset has pharmaceutical customers who are using the software in house, also.

"We have worked on projects which are now in the clinic, but all the information is confidential, so we can't talk about it in trying to attract funding or find a partner," said Leigh.

The FieldScreeen software has a current success rate for finding novel lead compounds of over 80 percent. This includes determining the bound conformation, selecting compounds for testing and finding a number of lead series for a popular peptide-ligand GPCR target, after screening just 88 compounds.

The company says most of these hits had no structural similarity to any known actives at the GPCR target, and thus could be developed at a distance from any competitive patents.

In another example of a GPCR with no known small molecule inhibitors, Cresset worked from the FieldPrint of the 30 amino-acid natural ligand and subsequently found 12 hits out of 44 small molecule compounds tested. The molecular weight of these hits ranged from 360-500 and all were non-peptide drug-like molecules amenable to medicinal chemistry.

"We have got the proof of principle for the technology. But when we do fee-for-service work we end up giving all the intellectual property back to the client," said Leigh. "Somehow we need to make the breakthrough to apply our proven technology to add value [to Cresset.]"

The Letchworth, UK-based company has set up a U.S. base and is trying to tap U.S. venture capitalists. In parallel, Leigh is looking for a partner to add in the biology needed to advance further up discovery and into development, and says Cresset would be receptive to a merger.

While the company is looking for relatively modest funding of up to $4 million, no one has bitten yet, although Leigh said the prospects are "looking a little better." At the same time Cresset is in early stage discussions with potential partners.

Cresset was set up in November 2001 with pounds 780,000 (then $1.5 million) seed funding from the medical charity the Wellcome Trust.