German firm Boehringer Ingelheim and Japan-based Sosei Group Corporation have entered a global collaboration and exclusive option-to-license agreement. At the centre is a joint mission to develop and commercialise Sosei Heptares’ portfolio of first-in-class GPR52 agonists, a novel G protein-coupled receptor (GPCR) target, with the intent to improve patient outcomes by simultaneously addressing positive, negative, and cognitive symptoms of schizophrenia.

Sosei Heptares will receive an upfront payment of EUR (€) 25 million from Boehringer Ingelheim upon signing and is eligible for an option exercise payment of EUR 60 million and further development, regulatory and commercialisation milestone payments totaling up to EUR 670 million plus customary tiered royalties for a clinical-stage asset on future Boehringer Ingelheim product sales.

Under the terms of the agreement, Boehringer Ingelheim has the exclusive option to license Sosei Heptares’ portfolio of GPR52 agonists following the completion of Sosei Heptares’ ongoing Phase 1 and subsequent Phase 1b trial and further Phase 2 enabling activities with HTL0048149, a first-in-class GPR52 agonist. Sosei Heptares will retain control and act as sponsor of these trials until option exercise, estimated in 2025. The licensed portfolio will include HTL0048149 as well as multiple differentiated back-up compounds designed by Sosei Heptares using its StaR® technology and structure-based drug design (SBDD) platform. 

GPR52 is an orphan G protein-coupled receptor (GPCR) highly expressed in the brain, especially in the striatum and the prefrontal cortex, and represents a potential emerging therapeutic target for a range of neurological and neuropsychiatric disorders.