Going commercial

TEL AVIV, Israel—Compugen Ltd. and DiscoveRx Corp. aretaking the wraps off a collaborative partnership that will focus on thecommercialization of novel Compugen-designed peptides to be matched withspecific G protein-coupled receptor (GPCR) targets utilizing DiscoveRx'sGPCR-related technologies.

The new agreement follows a successful pilot program betweenthe two companies. Financial terms of the agreement were not released.

The pilot project between the companies resulted inpromising initial results for a number of library peptides that were shown tomodulate specific GPCR targets, thus demonstrating both the library's potentialas a reservoir of therapeutically relevant peptides and the ability ofDiscoveRx's functional GPCR assays to identify novel peptide/GPCR targetinteractions.

Under the terms of the collaboration, DiscoveRx will utilizeits PathHunter Platform as well as its suite of additional proprietarycell-based GPCR assays and related technologies to match individual peptides inthe Compugen GPCR targeted peptide library with specific GPCR drug targets ofinterest to DiscoveRx's pharmaceutical company clients and others.

Following these activities, peptides of interest will beavailable for licensing from Compugen under milestone and royalty-bearingagreements. The parties have agreed to a revenue-sharing financial modelproviding different pre-arranged sharing percentages for each category ofrevenue anticipated by the collaboration.

According to Dr. Zurit Levine, vice president of researchand discovery at Compugen, the company's peptide library is suitable for screeninga wide range of GPCRs.

"DiscoveRx offers multiple GPCR screening assays and has abroad portfolio of GPCR cell lines and assays designed to detect GPCR signalingthrough different mechanisms," says Levine. "Therefore, DiscoveRx'scomprehensive GPCR assay portfolio and screening capabilities makes them anattractive partner for discovery of novel GPCR ligands within Compugen'slibrary."

Levine also notes that Compugen's peptide library containsmore than 900 peptides predicted to have a high likelihood of modulating GPCRtargets.

"It is known that newly discovered GPCR peptide ligands inthe past have shown a high probability of being successfully developed into newdrugs," says Levine. "Our unique and innovative approach to creating this peptidelibrary was developed using Compugen's proprietary GPCR Peptide LigandDiscovery Platform, which is based on our capability of identifying novelpeptide ligand agonists to GPCRs that could become drug candidates embeddedwithin the human proteome."

Levine further explains that the platform incorporates aproprietary model of the "peptidome," an in-silico prediction of putative human peptides, whichincludes thousands of novel predicted human peptide sequences, based onpredicting cleavage sites in precursor proteins.

"The discovery platform utilizes proprietarymachine-learning algorithms to analyze this peptidome and to identify peptideslikely to activate GPCRs. During the initial validation activities for thisplatform, three predicted peptides, CGEN-856, CGEN-855 and CGEN-25009, weresubsequently shown to have therapeutic potential in disease animal models ofcardiovascular, fibrotic and inflammatory conditions, which were published inleading scientific journals," says Levine. "In addition, Compugen has recentlyannounced that the Pulmonary Fibrosis Foundation will fund further studies toevaluate the potential of CGEN-25009 for treating lung fibrosis. Based on ourprevious findings of our technology, we believe this peptide library consistsof numerous potential new drugs targeting an important target class."

Anat Cohen-Dayag, Compugen's president and CEO, says thecompany is "focusing its discovery and development efforts towards addressingunmet medical needs in our focus areas of oncology and immunology through theuse of novel protein and antibody therapeutics."

"However, as part of the development and validationactivities associated with establishing our broadly applicable predictivediscovery capabilities, a number of very promising discoveries were made thathave significant potential in other areas," Cohen-Dayag says. "Therefore, inrecent months, we have been in various discussions for arrangements with otherorganizations to advance certain of these earlier discoveries, including a numberrelated to potential peptide therapeutics, largely without the need for furtherCompugen financial resources, such as this collaboration with DiscoveRx."

According to Dr. Pyare Khanna, CEO of DiscoveRx, thecollaboration is "a unique opportunity to address a key drug target classthrough a combination of DiscoveRx's most comprehensive and market-leading GPCRcell-based assay platforms, and Compugen's leading predictive capability forpeptide discovery."

Sailaja Kuchibhatla, senior vice president of businessdevelopment at DiscoveRx, says Compugen proved to be an attractive partner forthe collaboration because its in-silicopredictive models that utilize proprietary predictive platforms, algorithms andother computational biology capabilities have led to a collection ofproprietary molecules which can be taken through pre-IND programs.

"DiscoveRx offers next-generation, functional, cell-basedGPCR, kinase, NHR and pathway-signaling assay platforms that can, in anexpedited manner, provide functional validation as well provide greaterbiological insights into Compugen's proprietary collection," Kuchibhatla says."This joint collaborative model will allow third parties to engage incollaborations with both companies and thereby bring in functionally validatedproduct candidates for further development and commercialization, as well asvarious 'discovery-on-demand' arrangements, in most cases providing Compugenand DiscoveRx with potential milestone payments and royalties on product salesor other forms of revenue-sharing."