Omeros Identifies Small Molecules for Class B GPCR

              Omeros Identifies Small Molecules for Class B GPCR

- Expands "Unlocking" Capability Beyond Class A Orphan GPCRs -

PR Newswire

SEATTLE, Jan. 16, 2013

SEATTLE, Jan. 16, 2013 /PRNewswire/ -- Omeros Corporation (NASDAQ: OMER) today
announced that its proprietary Cellular Redistribution Assay (CRA) technology,
which to date has successfully "unlocked" 46 of the 80 total Class A orphan G
Protein-Coupled Receptors (GPCRs) for drug development, has identified small
molecules that interact with a Class B GPCR. Like the Class A GPCRs, Class B
receptors are important players in a broad range of disorders, having been
linked to various types of cancer (e.g., breast, brain, prostate, kidney,
liver, pancreatic and gastrointestinal); multiple sclerosis, attention
deficit-hyperactivity, learning and memory impairments, depression and other
neuropsychiatric disorders; multiple metabolic disorders including diabetes
and obesity; immunologic disorders; osteoporosis and infertility.

Of the 49 Class B GPCRs, 34 are orphans. An orphan receptor is one for which
there is no known ligand, or functionally active molecule. In developing drugs
against a given receptor, ligands are used as templates for medicinal
chemistry and, without them, drug development is extremely difficult.

In addition to continuing its screening of Class A orphan GPCRs, Omeros has
begun screening orphan and non-orphan Class B receptors. Of the non-orphan
Class B receptors, the Company will prioritize those for which there are
already commercially successful drugs – peptide or protein drugs that require
intravascular or intramuscular injection. 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 (PTH), a persistent
challenge. Despite the fact that oral agents are not available, the markets
for the Class B GPCR-targeting peptide drugs are large, with sales of PTH
drugs alone, for example, exceeding $1 billion annually. Omeros' CRA
technology finds functionally active small molecules for GPCRs, and could lead
to the development of oral medications for many of the Class B GPCRs.

"We continue to demonstrate the strength of our CRA technology and our team's
expertise in unlocking orphan GPCRs," stated Gregory A. Demopulos, M.D.,
chairman and chief executive officer of Omeros. "While we continue our efforts
to increase the number of our unlocked Class A receptors, establishing the
intellectual property position around each, our ability to identify small
molecules for Class B receptors further expands our GPCR platform and our
partnering opportunities. The promise of developing orally active drugs
against a class of receptors that have been, by necessity, largely served by
peptides and proteins, is exciting, particularly for those Class B GPCRs whose
biology has already been validated by marketed drugs."

Ongoing GPCR Program
Omeros is screening orphan and difficult-to-drug Class A and Class B GPCRs
against its small-molecule chemical libraries using its proprietary,
high-throughput cellular redistribution assay (CRA). The CRA detects receptor
antagonists, agonists, inverse agonists and allosteric modulators for a given
GPCR without requiring the receptor's ligand or any knowledge of the
receptor's signaling pathway(s). Omeros has announced that it has identified
and confirmed sets of compounds that interact selectively with 46 Class A
orphan receptors linked to metastatic melanoma (GPR19), esophageal squamous
cell carcinoma and obesity-related type-2 diabetes (GPR39), hepatocellular
carcinoma (GPR80), several types of cancer (GPR65/TDAG8), squamous cell
carcinoma (GPR87), ovarian cancer (GPR150), 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" and bipolar disorder (GPR50), anxiety
disorders (GPR31), schizophrenia (GPR52, GPR153), autism (GPR63), bipolar
disorder and schizophrenia (GPR78), memory and inflammatory conditions
(GPR83), psychotic and metabolic disorders (GPR27, GPR85, GPR173), cognition
(GPR151), cognitive impairments (MAS1), inflammatory responses (GPR32),
obesity and diabetes (GPR21), appetite control (GPR82, GPR101), immunological
disorders (CCRL2), rheumatoid arthritis and HIV-mediated enteropathy (GPR15),
respiratory and immune disorders (GPR141), humoral immunity (GPR183), multiple
sclerosis (GPR17), osteoarthritis (GPR22), motor control (GPR139), congenital
cataracts and birth defects of the brain and spinal cord (GPR161), regulation
of hematopoietic stem cell differentiation (GPR171), cancer stem cells and the
self-renewal and maintenance of adult stem cells (LGR4), long-term wound
repair, including the formation of new hair follicles (LGR6) and pain (MRGE).
In addition, Omeros has unlocked GPR20, GPR45, GPR135, GPR162, MRGF and OPN5,
which have not yet been definitively tied to any specific indications but are
expressed preferentially in the gastrointestinal tract (GPR20), brain (GPR45,
GPR135 and GPR162) and eye, brain, testes, spinal cord (OPN5) and dorsal root
ganglia (MRGF).

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 80
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, antagonists and allosteric modulators for orphan and
difficult-to-drug 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, OMS302 for lens replacement surgery and OMS103HP
for arthroscopy, 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 five 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, Omeros' expectations regarding its planned screening of GPCRs; and
that Omeros may have capability, through its GPCR program, to 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 November 9, 2012. 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

Contact: Jennifer Cook Williams, Cook Williams Communications, Inc., Investor
and Media Relations, +1-360-668-3701, jennifer@cwcomm.org
 
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