Omeros Identifies Small Molecules for Class B GPCR
- Expands "Unlocking" Capability Beyond Class A Orphan GPCRs -
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."