Adding Six More, Omeros Now Has a Total of 33 Unlocked Orphan GPCRs in its Portfolio
SEATTLE, Feb. 29, 2012 /PRNewswire/ — Omeros Corporation (NASDAQ: OMER) today announced that it has identified compounds that functionally interact with each of the following six orphan G protein-coupled receptors (GPCRs): GPR17, GPR153, CCRL2, LGR4, LGR6 and OPN5. Without compounds that functionally interact with orphan GPCRs, developing drugs targeting those receptors is extremely difficult. Omeros has now unlocked 33 of them, representing over 40 percent of the Class A orphan GPCRs. There are approximately 120 orphan GPCRs and Omeros expects to unlock a large percentage of them, focusing first on Class A orphan GPCRs.
GPR17 is a novel target tied to multiple sclerosis. GPR153 is associated with schizophrenia, and CCRL2 is connected to immunological disorders, such as rheumatoid arthritis. LGR4 is linked to cancer stem cells and the self-renewal and maintenance of adult stem cells. LGR4 is also tied to bone disorders, such as osteoporosis. LGR6 is expressed in the hair follicle stem cells and is involved in long-term wound repair, including the formation of new hair follicles. OPN5 is a recently discovered photoreceptor for ultraviolet light, but its physiological role is currently unknown. Omeros is in the process of filing broad patent applications around its unlocked orphan GPCRs and compound optimization efforts are in progress.
“We continue to advance rapidly through the Class A orphans and, by the end of 2012, we plan to have screened them all using our proprietary Cellular Redistribution Assay,” said Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. “For each of these receptors, the compounds uniquely identified by Omeros represent keys to drug development, and we believe that Omeros exclusively controls those keys. In parallel with our successful screening efforts, we are building our patent position for each of our unlocked orphans with the goal of protecting and capitalizing on our discoveries.”
Ongoing GPCR Program
Omeros is screening orphan GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput cellular redistribution assay (CRA). The CRA detects receptor antagonists, agonists and inverse agonists. Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with 33 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), ovarian and prostate cancer (OGR1), arterial stiffness (GPR25), sleep disorders (OPN4), cognitive disorders (GPR12), torpor or “suspended animation” (GPR50), anxiety disorders (GPR31), schizophrenia (GPR52, GPR153), bipolar disorder and schizophrenia (GPR78), psychotic and metabolic disorders (GPR27, GPR85, GPR173), cognitive impairments (MAS1), inflammatory responses (GPR32), obesity and diabetes (GPR21), appetite control (GPR101), immunological disorders (CCRL2), rheumatoid arthritis and HIV-mediated enteropathy (GPR15), respiratory and immune disorders (GPR141), multiple sclerosis (GPR17), motor control (GPR139), congenital cataracts and birth defects of the brain and spinal cord (GPR161), cancer stem cells and the self-renewal and maintenance of adult stem cells (LGR4) and long-term wound repair, including the formation of new hair follicles (LGR6). In addition, Omeros has unlocked GPR20, GPR135 and OPN5, which have not yet been tied to any indications but are expressed preferentially in the gastrointestinal tract (GPR20), brain (GPR135) and eye, brain, testes and spinal cord (OPN5).
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(TM) 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.
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 GPR17, GPR153, CCRL2, LGR4, LGR6 and OPN5; Omeros’ ability to obtain broad patent protection for the orphan GPCRs that it has unlocked; 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