Omeros identifies orphan GPCR compound that potentiates tumor-killing activity of doxorubicin

Omeros Corporation (Nasdaq: OMER), a biopharmaceutical company committed to discovering, developing and commercializing products focused on inflammation and disorders of the central nervous system, today announced that a compound identified by the Company as an antagonist of GPR87, an orphan GPCR recently unlocked for drug development by Omeros and linked to squamous cell carcinoma, potentiates the tumor-killing activity of doxorubicin (Adriamycin), a widely used chemotherapeutic agent. This is the first compound in a series of GPR87 antagonists exclusively identified by Omeros that the Company has evaluated in proof-of-concept models. Omeros is currently initiating medicinal-chemistry optimization of the compound.

Adriamycin is a potent chemotherapy drug commonly used to treat leukemias and Hodgkin's lymphoma, as well as cancers of the breast, lung, stomach, bladder, ovaries and thyroid, soft tissue sarcoma, multiple myeloma, and other types of cancer. While very effective in killing cancer cells, Adriamycin's dosing is limited by its life-threatening damage to heart muscle. The ability to reduce Adriamycin's dosing and its dose-related toxicity, while maintaining its cancer lethality, would be a significant advance in the treatment of multiple types of cancer.

"We are excited by these recent data further confirming that our Cellular Redistribution Assay identifies compounds that interact with orphan GPCRs and affect their function," said Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. "Despite not yet having optimized this GPR87 antagonist, the compound demonstrates the expected benefit of potentiating tumor-cell killing by Adriamycin. We are eager to evaluate our other GPR87 antagonists, as well as the compounds that we identified as antagonists of GPR85 and GPR101, and look forward to screening the remaining orphans."