Omeros Unlocks Orphan GPCR Family Linked to Metabolic and Psychotic Disorders
SEATTLE, May 31, 2011 /PRNewswire/ — Omeros Corporation (NASDAQ: OMER) today reported that it has identified compounds that interact with orphan G protein-coupled receptors (GPCRs) GPR27 and GPR173. These receptors, together with GPR85, an orphan GPCR that Omeros previously unlocked, form the SREB (Super Conserved Receptor Expressed in Brain) family, a unique and evolutionarily conserved family of orphan GPCRs thought to be critical in regulating neural integrity. The SREB family is linked to metabolic and psychotic disorders such as obesity and schizophrenia.
Omeros also announced today that it has identified compounds that interact with GPR139, an orphan GPCR primarily located in the central nervous system that may play a role in motor control. In total, Omeros has already unlocked eight, or approximately 10 percent, of the 81 Class A 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, which expects to unlock a large percentage of these for drug development, is initially targeting Class A orphan GPCRs.
“We have now identified compounds for 10 percent of the Class A orphan GPCRs,” said Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. “This includes all of the known SREBs, one of the most highly conserved families of GPCRs – an achievement that could facilitate the development of new drugs targeting these receptors for the treatment of important metabolic and psychotic disorders.”
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 eight orphan receptors linked to squamous cell carcinoma (GPR87), pancreatic cancer (GPR182),metabolic and psychotic disorders(GPR27, GPR85, GPR173), appetite control (GPR101), cognitive disorders (GPR12) and motor control (GPR139). 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 ClaritinÃ‚® (allergy), ZantacÃ‚® (ulcers and reflux), OxyContinÃ‚® (pain), LopressorÃ‚® (high blood pressure), ImitrexÃ‚® (migraine headache), ReglanÃ‚® (nausea) and AbilifyÃ‚® (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, 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, bleeding 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’ expectations regarding its ability unlock orphan GPCRS and add a large number of new drug targets and their corresponding compounds to the market. 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 May 10, 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