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Omeros Unlocks Orphan GPCRs Linked to Pancreatic Cancer and Cognitive Disorders
Date:3/2/2011

SEATTLE, March 2, 2011 /PRNewswire/ -- Omeros Corporation (Nasdaq: OMER) today announced that it has identified compounds that interact selectively with two orphan G protein-coupled receptors (GPCRs) linked to pancreatic cancer (GPR182) and cognitive disorders (GPR12). Together with the three previously unlocked orphans linked to squamous cell carcinoma (GPR87), obesity (GPR85) and appetite control (GPR101), Omeros has now successfully unlocked five orphan GPCRs.

GPCRs represent the premier family of drug targets, with more than 30 percent of currently marketed drugs targeting only 46 GPCRs. There are approximately 120 orphan GPCRs, and Omeros expects to unlock a large percentage of these for drug development. Omeros also announced today that it has cloned approximately 90 percent of the 81 Class A orphan GPCRs into the vector of its proprietary cellular redistribution assay (CRA). The Company is advancing these receptors toward screening in its CRA.

"The progress in our GPCR program has been rapid and we remain on track to screen all of the Class A orphan GPCRs by mid-2012," stated Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. "Out of the seven receptors screened against only a portion of our compound libraries, we have so far identified multiple small molecules for each of five orphans, demonstrating the power of our proprietary assay to open orphan GPCRs to drug development. We have nearly completed the preparatory steps for large-scale throughput, including generation of clones and constructs as well as integrating our automation capabilities, and we expect that we will soon reach our full screening rate."

Ongoing GPCR Program

Omeros has begun screening orphan GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput CRA. Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with five orphan receptors linked to squamous cell carcinoma (GPR87), pancreatic cancer (GPR182), obesity (GPR85), appetite control (GPR101) and cognitive disorders (GPR12). The CRA detects receptor antagonists and agonists. Antagonists comprise the majority of marketed drugs, and all of the compounds identified so far by Omeros are antagonists.

About G Protein-Coupled Receptors

GPCRs, which mediate key physiological processes in the body, are one of the most valuable families of drug targets. According to Insight Pharma Reports, GPCR-targeting drugs represent 30 to 40 percent of marketed pharmaceuticals. Examples include Claritin® (allergy), Zantac® (ulcers and reflux), OxyContin® (pain), Lopressor® (high blood pressure), Imitrex® (migraine headache), Reglan® (nausea) and Abilify® (schizophrenia, bipolar disease and depression) as well as all other antihistamines, opioids, alpha and beta blockers, serotonergics and dopaminergics.  

The industry focuses its GPCR drug discovery efforts mostly on non-sensory GPCRs. Of the 363 total non-sensory GPCRs, approximately 240 have known ligands (molecules that bind the receptors) with nearly half of those targeted either by marketed drugs (46 GPCRs) or by drugs in development (about 70 GPCRs). There are approximately 120 GPCRs with no known ligands, which are termed "orphan GPCRs." Without a known ligand, drug development for a given receptor is extremely difficult.

Omeros uses its proprietary high-throughput CRA to identify small-molecule agonists and antagonists for orphan GPCRs, unlocking them to drug development. Omeros believes that it is the first to possess the capability to unlock orphan GPCRs in high-throughput, and that currently there is no other comparable technology. Unlocking these receptors could lead to the development of drugs that act at these new targets. There is a broad range of indications linked to orphan GPCRs including cardiovascular disease, asthma, diabetes, pain, obesity, Alzheimer's disease, Parkinson's disease, multiple sclerosis, schizophrenia, learning and cognitive disorders, autism, osteoporosis, osteoarthritis and several forms of cancer.

About Omeros Corporation

Omeros is a clinical-stage biopharmaceutical company committed to discovering, developing and commercializing products focused on inflammation, bleeding and disorders of the central nervous system. The Company's most clinically advanced product candidates are derived from its proprietary PharmacoSurgery™ platform designed to improve clinical outcomes of patients undergoing a wide range of surgical and medical procedures. Omeros has six ongoing clinical development programs, including four from its PharmacoSurgery™ platform, the most advanced of which is in a Phase 3 clinical program, and two from its addiction franchise. Omeros may also have the near-term capability, through its GPCR program, to add a large number of new drug targets and their corresponding compounds to the market. Behind its clinical candidates and GPCR platform, Omeros is building a diverse pipeline of protein and small-molecule preclinical programs targeting inflammation, bleeding and central nervous system disorders.

Forward-looking Statements

This press release contains forward-looking statements as defined within the Private Securities Litigation Reform Act of 1995, which are subject to the "safe harbor" created by those sections. Forward-looking statements are based on management's beliefs and assumptions and on information available to management only as of the date of this press release and include Omeros' expectation that it will unlock a large percentage of the orphan GPCRs, the Company's ability to screen all of the Class A orphan GPCRs by mid-2012, Omeros' expectation that it will soon reach its full screening rate of orphan GPCRs, Omeros' belief that unlocking these receptors could lead to the development of drugs that act at these new targets, and Omeros' belief that it may also have the near-term capability, through its GPCR program, to add a large number of new drug targets and their corresponding compounds to the market. Omeros' actual results could differ materially from those anticipated in these forward-looking statements for many reasons, including, without limitation, the risks, uncertainties and other factors described under the heading "Risk Factors" in the Company's Quarterly Report on Form 10-Q filed with the Securities and Exchange Commission on November 4, 2010. Given these risks, uncertainties and other factors, you should not place undue reliance on these forward-looking statements, and the Company assumes no obligation to update these forward-looking statements publicly, even if new information becomes available in the future.


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