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A trio of leads for a hopeful future
February 2012
by Jeffrey Bouley  |  Email the author


JERUSALEM—Biopharmaceutical development company BioLineRx Ltd. has entered into a collaboration agreement with fellow Israeli company Compugen Ltd. for early- to mid-stage development of mutually selected drug candidates for the treatment of various diseases, ranging from acute and chronic inflammatory diseases to cardiac diseases, retinopathy and cancer.  
Under the deal, Tel Aviv-based Compugen is providing promising drug candidates that were identified using its predictive in-silico drug discovery platforms. For its part, BioLineRx is to develop these candidates through Phase II clinical trials, with an eye toward eventually licensing them to pharmaceutical companies for advanced clinical development and commercialization.  
The collaboration is getting its start with the selection of three Compugen-discovered peptides. Two of the peptides, named CGEN-855 and CGEN-856, will enter BioLineRx's main product pipeline as BL-7070 and will focus on preventing and treating cardiovascular diseases by controlling inflammation and reducing hypertension. The third peptide, CGEN-25017, will enter BioLineRx's pipeline as BL- 8010 and is intended for the treatment of diseases characterized by excessive growth of new blood vessels, such as retinopathy and cancer. All three have already undergone proof-of-concept animal studies.  
Both parties will continue to evaluate other Compugen-discovered drug candidates for development by BioLineRx.
"Part of the collaborative framework agreement is to put together a committee made up of people from both companies—on the business end and on the science side—because there is a real interest on both sides to interact more proactively," Josh Hexter, BioLineRx's executive director of corporate in-licensing, tells ddn, adding that in years past, BioLineRx had explored possible one-off projects with Compugen that never took off. "When we did due diligence for this more strategic and long-term kind of collaboration, we looked through what they had in their discovery pipeline and flushed through it to find some promising peptides, but we're also interested in sitting down with them to outline targets and indications of interest to us and put those through their platform to maybe get some other interesting assets."  
"Joining forces with the proven drug validation and development skills of BioLineRx to advance the development of such previously discovered promising Compugen peptide discoveries served as a natural fit for both companies," Tsipi Keren-Lehrer, Compugen's director of business development, tells ddn. "This is also the reason why the parties will continue to evaluate other Compugen-discovered drug candidates for development by BioLineRx. The business model of our company is to maximize the number of Compugen's product candidates in the pipelines of pharma and biotech companies under milestones, royalties and other revenue-sharing arrangements. We therefore constantly look for excellent partners in order to advance the development and commercialization of our assets."  
The partnership is made all the more perfect and promising, Hexter notes, by the fact that "Compugen is great at discovery but doesn't have much of a development arm, whereas we're good at development but don't really have a discovery arm. We see this deal as highly strategic and co-development in nature; we won't just sit on our hands and wait for another list of peptides, but rather see how we can best use Compugen's platform to find new leads to take forward."
In the news release about the deal, BioLineRx CEO Dr. Kinneret Savitsky said much the same, noting, "This mutually beneficial agreement is in keeping with our company strategy of seeking promising therapeutic candidates for our product pipeline and developing them through Phase II clinical trials."  
Compugen's president and CEO, Dr. Anat Cohen-Dayag, added that as part of his company 's process of establishing its broadly applicable predictive discovery capabilities, "a number of promising potential therapeutic peptides and other potential drug candidates were discovered that are not in these main areas of focus. The goal of this collaboration with BioLineRx and others which have been, or will be, announced, is to advance certain of these promising discoveries, without the need for further Compugen financial resources, but with Compugen sharing in the value created."
CGEN-855 is a novel peptide agonist of the FPRL1 G-protein coupled receptor (GPCR), discovered by Compugen's GPCR Peptide Ligand Discovery Platform. FPRL1 is expressed by various immune system cells, and its activation promotes resolution of inflammation, leading to pronounced anti-inflammatory activity. Accordingly, CGEN-855 has shown anti-inflammatory activity when tested in animal models of acute inflammation and has exhibited a cardioprotective effect in models of acute myocardial infarction in mice and rats. CGEN-855 was also shown to be beneficial in an animal model of inflammatory bowel disease. These results support the therapeutic potential of CGEN-855 in treating acute and chronic inflammation, as well as cardiovascular diseases.  
CGEN-856 is a novel ligand of the MAS GPCR receptor, one of the key components of the renin-angiotensin system which controls blood pressure and water balance in the body. This peptide was discovered by Compugen's GPCR Peptide Ligand Discovery Platform. CGEN-856 induced relaxation of rat and murine aortas, reduced in-vivo cardiac remodeling induced by isoproterenol or ischemia and displayed anti-hypertensive effects as well as cardiac and renal anti-fibrotic effects. CGEN-856 may thus be a useful therapeutic agent in conditions such as hypertension, heart failure, cardiac remodeling, myocardial infarction, renal fibrosis and other cardiovascular pathologies.  
CGEN- 25017 is a novel peptide antagonist of the Angiopoietin/Tie-2 pathway that is crucial for angiogenesis, blood vessel maturation and vascular endothelium integrity. The peptide has shown positive therapeutic effects in an animal model of retinopathy. CGEN-25017, which was initially discovered using Compugen's Disease-Associated Conformation Blockers Discovery Platform, had previously demonstrated significant inhibitory activity in an animal model of retinopathy and in two other models of angiogenesis. Based on its anti-angiogenic properties, CGEN-25017 has potential therapeutic utility for additional diseases involving pathological angiogenesis such as cancer and inflammatory conditions, including psoriasis and rheumatoid arthritis.   

Compugen in $8 million research deal with Baize Investments  
TEL AVIV, Israel—Compugen Ltd. also recently announced an $8 million research funding agreement with Baize Investments Ltd., a private corporation also based in Israel that invests in innovative medical technologies.   The funding agreement follows an earlier pact between the two parties formed in December 2010, in which Compugen received $5 million in support of the initiation of its monoclonal antibody (mAb) pipeline program.  
Baize will receive a financial interest in therapeutic mAb product candidates to be developed against 12 specified Compugen-discovered targets in the field of oncology, provided that any such mAb product candidates either achieves a successful animal disease model during the next three years, and/or is licensed out to third parties for final development and commercialization. Baize is entitled to a percentage of future payments received by Compugen from third parties from any out-licensing for further development and/or commercialization. In addition, Baize has the right, during the first quarter of 2014, to waive its rights to receive all such future payments in exchange for 1.45 million Compugen ordinary shares.  
Of Compugen's pipeline, Murray Goldman, Baize's chairman, stated, "This is anticipated to lead to significant new therapeutic candidates addressing key unmet needs in cancer treatment, which could meaningfully contribute to the well-being of humanity." 

Code: E021207



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