Merck, a leading science and technology company, has announced a licensing agreement with US-based firm Inspirna, Inc. for ompenaclid (RGX-202), a first-in-class oral inhibitor of the creatine transport channel SLC6A8, and SLC6A8-targeting follow-on compounds. Ompenaclid is currently being evaluated in a Phase II study for the second-line treatment of RAS-mutated (RASmut) advanced or metastatic colorectal cancer (mCRC).

Ompenaclid is a first-in-class oral inhibitor of the creatine transport channel SLC6A8. Data from the Phase Ib/II study of ompenaclid in combination with FOLFIRI and bevacizumab showed encouraging efficacy and safety for second-line treatment of RASmut mCRC. 

The collaboration with Inspirna builds on Merck’s long-standing commitment to the colorectal cancer community. 2024 marks the 20th anniversary of the introduction of ERBITUX^®, for which the company has marketing rights outside the U.S. and Canada, as a backbone treatment in mCRC; today, multiple active clinical trials continue to evaluate ERBITUX^® in this disease. The company is also developing M9140, a CEACAM5-targeting antibody-drug conjugate with an exatecan payload currently being evaluated in an ongoing Phase Ia/b study in patients with mCRC.

Under the terms of the license agreement, Merck will receive an exclusive license to ompenaclid outside of the US and an option to co-develop and co-promote ompenaclid in the US. Furthermore, the parties agreed to collaborate on Inspirna’s SLC6A8 follow-on compounds for which Inspirna will retain US co-development and co-commercialization rights. Inspirna will receive an upfront payment of $45 million.