HTS assay has reportedly already identified modulators of three orphan receptors.

Omeros received a $20 million investment from Vulcan Capital and a $5 million grant from Washington State’s Life Sciences Discovery Fund to support further development of its GPCR drug discovery program. The Vulcan deal means Omeros can exercise its existing option to purchase Patobios’ high-throughput screening (HTS) platform for orphan GPCRs for C$7.8 million in cash and $3 million in Omeros stock.

Both Vulcan and Washington’s Life Sciences Discovery Fund will, in return for their funding, have rights to a percentage of the net proceeds generated by Omeros’ program. The level of tiered payments will decrease as cumulative net proceeds reach specific thresholds. Vulcan has in addition been issued with three five-year warrants to purchase Omeros common stock. Each warrant is for 133,333 shares, with exercise prices of $20, $30, and $40 per share, respectively.

For the last two years, Omeros has held an exclusive option to purchase a cellular redistribution assay from Canadian firm Patobios. Omeros believes is the only technology capable of identifying agonists and antagonists of orphan GPCRs in a high-throughput manner. During the option period, Omeros has been able to use the technology to screen up to three sets of five orphan GPCRs. On completion of the C$10.8 million technology purchase agreement the firm will no longer have any milestone, royalty, or other payment obligations to Patobios.

Omeros reached a milestone in the GPCR program back in June, when it reported identifying compounds that interact with three orphan GPCRs linked to cancer, metabolic disorders, and appetite control.

Omeros says estimates suggest that GPCR-targeting drugs represent about 30–40% of the $700 billion in annual worldwide drug sales. It suggests that of the 363 nonsensory GPCRs, about 240 have known ligands. Marketed drug target 46 of these, and there are drugs currently in development that target another 70. Omeros believes that over 65 of the remaining 120 or so orphan GPCRs could represent druggable targets.

The firm’s GPCR research is at a relatively early stage in comparison with its existing clinical pipeline. This is headed by products developed using its PharmacoSurgery™ platform. The PharmacoSurgery approach is based on developing formulations of FDA-approved generic drugs that can be included in standard surgical irrigation solutions to help pre-empt and reduce surgical-related trauma and promote healing in patients undergoing procedures including arthroscopy, ophthalmology, and urology procedures.

Lead product, OMS103HP, is undergoing clinical programs at orthopedic sports medicine centers throughout the U.S. and Canada. The Phase III trial is evaluating the safety and ability of OMS103HP to improve postoperative joint function and reduce pain following arthroscopic anterior cruciate ligament reconstruction surgery. A second trial is evaluating whether OMS103HP reduces pain and improves postoperative joint function following arthroscopic partial meniscectomy surgery.

Omeros is separately focused on the development of treatments for CNS disorders. Its lead addition treatment/prevention candidate has completed a Phase II clinical trial.

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