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Compugen Announces Positive Therapeutic Effects of Relaxin Receptor in Pulmonary Fibrosis

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Compugen has announced that CGEN-25009, a novel peptide that previously demonstrated the ability to activate the Relaxin receptor LGR7 (RXFP1) in cell based assays, has shown positive therapeutic effects in an animal model of pulmonary fibrosis.

The Relaxin receptor is the third G-protein coupled receptor (GPCR) for which Compugen-discovered peptide ligands have shown therapeutic potential in disease models.

“Following two weeks of administration of the CGEN-25009 peptide to mice induced with lung fibrosis, there was a complete reduction in the fibrosis. This improvement was evident both by histology staining and by measuring the Pressure at the Airway Opening (PAO), where levels were comparable to those observed in healthy mice,” said Dr. Anat Cohen-Dayag, vice president, research and development.

“These results suggest that CGEN-25009 prevents pulmonary fibrosis in a disease animal model and therefore could have a potential therapeutic utility to treat pulmonary fibrosis and other fibrosis related conditions, such as chronic renal failure.”

Professor Daniele Bani from the University of Florence, Italy, who performed the animal study and is a recognized world expert in this field with numerous publications on Relaxin’s biology and pathway added, “To my knowledge, this would be the first report on the therapeutic effectiveness of an analogue of Relaxin. In view of the increasing interest in Relaxin as a possible drug and considering the problems inherent in producing enough of this hormone at a reasonably low cost, it could be foreseen that such information would be enthusiastically welcomed.”

Pulmonary fibrosis is a devastating incurable condition, the cause for which is unknown in most cases. It is estimated to affect more than five million people worldwide with tens of thousands of new cases every year in the United States. More than 60% of patients diagnosed with the condition survive less than five years.

CGEN-25009, along with two other Relaxin related peptides, CGEN 25010 and 25011, were among the first peptide ligands predicted and selected utilizing Compugen’s GPCR Ligand Discovery Platform. These peptides were first presented in May 2008 at the 5th International Conference on Relaxin and Related Peptides. Compugen’s initial results suggested that CGEN-25009 has biological activities similar to those of Relaxin, which are now further supported by the in-vivo findings.