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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 cellular redistribution assay (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 conduct high-throughput drug discovery for orphan GPCRs, and that currently there is no other existing high-throughput technology able to "unlock" orphan GPCRs. 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.

Omeros has begun screening orphan GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput CRA. In addition to Class A orphan GPCRs, we have also begun screening orphan and non-orphan Class B receptors. Class B GPCRs have large extracellular domains and their natural ligands are generally large peptides, making the development of orally active, small-molecule drugs against these receptors, such as glucagon and parathyroid hormone, a persistent challenge. Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with the following orphan receptors:

GPCR Metabolic & Cardiovascular Indications GPCROncology Indications
GPR12Obesity, Cognitive Impairments GPR19 Melanoma, Lung Cancer
GPR21 Obesity, Diabetes GPR20 Gastro-Intestinal Stromal Tumors, Acute Myeloid Leukemia
GPR22 Cardiovascular Diseases, Anxiety GPR65 Renal Cell Carcinoma, Ovarian Cancer, Inflammation
GPR25 Arterial Stiffness GPR68 Ovarian Cancer, Prostate Cancer, Osteoporosis
GPR37L1 Hypertension GPR80 Hepatocellular Carcinoma
GPR39 Diabetes GPR87 Squamous Cell Carcinoma
GPR50 Metabolic Disorders GPR150 Ovarian Cancer
GPR61 Eating Disorders GPR161 Breast Cancer, Congenital Cataracts & Birth Defects
GPR82 Appetite, Body Weight GPR174 Melanoma, Grave’s Disease
GPR101 Eating Disorders LGR4 Cancer Stem Cells, Bone Diseases
GPR132 Atherosclerosis LGR5 Cancer Stem Cells, Esophageal Adenocarcinoma
GPR146 Dyslipidemia, Diabetes P2Y8 Leukemias, Lymphomas
GPR171 Eating Disorders  
GPR176 Atherosclerosis
SREB1/GPR27 Diabetes, Schizophrenia
GPCRCNS Indications GPCR Miscellaneous Indications
GPR17 Myelin Disorders, Multiple Sclerosis GPR15HIV Enteropathy, Rheumatoid Arthritis
GPR31Anxiety Disorders GPR32 Acute Inflammatory Responses
GPR37 Parkinson’s Disease GPR83 Autoimmune Diseases, PTSD
GPR52Schizophrenia GPR183Humoral Immunity
GPR63Autism CCRL2Rheumatoid Arthritis
GPR78Bipolar Disorder, Schizophrenia LGR6Hair Follicle Stem Cells, Wound Repair
GPR139 Motor Disorders GPCRs with Unknown Indications
GPR151 Cognition, Mood Disorders, Pain
GPR45 GPR182
GPR153 Schizophrenia
MAS1 Cognitive Impairments
OPN4 Circadian Rhythm, Sleep Disorders
SREB2/GPR85 Schizophrenia, Obesity
SREB3/GPR173 Schizophrenia, Obesity

In parallel, Omeros is executing on its intellectual property strategy to protect each unlocked target through a multipronged approach directed to compound structures, uniquely identified signaling pathways and associated therapeutic indications. Collectively, this approach provides Omeros the opportunity to establish broad and enforceable protection for each unlocked receptor.


We are optimizing compounds against GPR17, a G protein-coupled receptor (GPCR) which is linked to myelin formation. Myelin is an insulating layer rich in lipids and proteins that forms a sheath around the nerve fibers, which is essential for the proper functioning of the nervous system. Loss of the myelin sheath is the hallmark of several diseases, including multiple sclerosis, acute disseminated encephalomyelitis, Neuromyelitis Optica, transverse myelitis, chronic inflammatory demyelinating polyneuropathy, Guillain-Barré syndrome, central pontine myelinosis, inherited demyelinating diseases such as leukodystrophy, and Charcot-Marie-Tooth disease. We believe GPR17 inhibitors have the potential to promote remyelination and improve the outcome of these diseases as well as traumatic brain injury and spinal cord injury, conditions that have been associated with GPR17.

Discovering GPR17 inhibitors has previously been challenging to the pharmaceutical industry because this receptor is an orphan GPCR, i.e., its natural ligand is not known, as discussed below. However, using our proprietary CRA, which allows compound screening against orphan GPCRs without knowledge of a given receptor's natural ligand, we have been able to identify over 120 compounds that functionally interact with GPR17.

Patent Position

As of February 28, 2015, we owned five issued patents and 16 pending patent applications in the U.S., and 43 issued patents and eight pending patent applications in foreign markets, which are directed to previously unknown links between specific molecular targets in the brain and a series of CNS disorders, our cellular redistribution assay and other research tools that are used in our GPCR program and to orphan GPCRs and other GPCRs for which we have identified functionally interacting compounds using our CRA.