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Omeros Announces it has Unlocked 30 Percent of Class A Orphan GPCRs

SEATTLE, Jan. 10, 2012 /PRNewswire/ -- Omeros Corporation (NASDAQ: OMER) today reported that it has identified compounds that interact selectively with each of GPR25, GPR32, GPR80, GPR135 and MAS1, bringing the total number of orphan G protein-coupled receptors (GPCRs) unlocked by Omeros to 23, representing 30 percent of the Class A orphan GPCRs. To date, the number of orphans unlocked by Omeros for drug development equals half of the total number of GPCRs currently targeted by more than 30 percent of all marketed drugs. There are approximately 120 orphan GPCRs and Omeros expects to unlock a large percentage of them, focusing first on Class A orphan GPCRs.

GPR25 is linked to arterial stiffness, which is associated with atherosclerosis, myocardial infarction and stroke. GPR32 is tied to acute inflammation. GPR80 is linked to hepatocellular carcinoma and MAS1 to cognitive impairment, a central component of debilitating disorders such as Alzheimer's and other dementias. No potential indications have yet been linked to GPR135, although it is expressed throughout the body and widely, and preferentially, in the brain. Omeros is in the process of filing broad patent applications around its unlocked orphan GPCRs and compound optimization efforts are underway.

"Using our proprietary high-throughput assay, we are moving rapidly through the 77 Class A orphans and expect to complete screening of them all in 2012," said Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. "We believe the compounds that we have uniquely identified for our unlocked orphan GPCRs enable the development of drug candidates selectively targeting each of those receptors, and we are working diligently to advance, protect and capitalize on our discoveries."   

Ongoing GPCR Program

Omeros has begun screening orphan GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput cellular redistribution assay (CRA). Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with 23 orphan receptors linked to metastatic melanoma (GPR19), esophageal squamous cell carcinoma and obesity-related type-2 diabetes (GPR39), hepatocellular carcinoma (GPR80), squamous cell carcinoma (GPR87), pancreatic cancer (GPR182), acute lymphoblastic leukemia (P2Y8/P2RY8), arterial stiffness (GPR25), sleep disorders (OPN4), cognitive disorders (GPR12), anxiety disorders (GPR31), bipolar disorder and schizophrenia (GPR78), psychotic and metabolic disorders (GPR27, GPR85, GPR173), cognitive impairments (MAS1), inflammatory responses (GPR32), appetite control (GPR101), rheumatoid arthritis and HIV-mediated enteropathy (GPR15), respiratory and immune disorders (GPR141), motor control (GPR139) and congenital cataracts and birth defects of the brain and spinal cord (GPR161). In addition, Omeros has unlocked GPR 20 and GPR135, which have not yet been tied to any indications but are expressed preferentially in the gastrointestinal tract and brain, respectively. The CRA detects receptor antagonists and agonists. Antagonists comprise the majority of marketed drugs, and all of the compounds characterized 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 targeting inflammation, coagulopathies 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 four ongoing clinical development programs. 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, coagulopathies 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. These statements include, but are not limited to, statements regarding Omeros' expectation regarding its ability unlock orphan GPCRs and add a large number of new drug targets and their corresponding compounds to the market; the disorders that could potentially be treated by drugs that target unlocked orphan receptors, including GPR25, GPR32, GPR80, GPR135 and MAS1; Omeros' ability to obtain broad patent protection for the orphan GPCRs that it has unlocked; the pharmaceutical industry's ability to design proprietary compounds that interact with these receptors; and the Company's ability to complete the screening of all Class A orphans by the end of 2012. 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. 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 8, 2011. 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.

SOURCE Omeros Corporation
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