Boehringer Ingelheim and Sosei Heptares entered a global collaboration and exclusive option-to-license agreement to develop and commercialize Sosei Heptares’ portfolio of first-in-class GPR52 agonists, a novel G protein-coupled receptor (GPCR) target, to improve patient outcomes by simultaneously addressing positive, negative, and cognitive symptoms of schizophrenia.
 
Schizophrenia is affects about 1 in 100 people worldwide. It is characterized by three clusters of symptoms: such as psychosis, delusions and hallucinations, social withdrawal and apathy, and attention, planning and memory deficits. While ‘positive’ symptoms can be stabilized with antipsychotics, some of which can have side effects, there are currently no approved medicines for ‘negative’ or cognitive symptoms.
 
The development of a new schizophrenia treatment targeting GPR52 has the potential to address all three aspects of schizophrenia providing a novel precision treatment. This is based on the location of the receptor in the two areas of the brain that drive the positive (the striatum) and the negative and cognitive symptoms (the prefrontal cortex). The GPR52 agonism calms the striatum while boosting frontal cortical function.
 
Sosei Heptares will receive €25 million upfront from Boehringer Ingelheim upon signing and is eligible for an option exercise payment of €60 million and further development, regulatory and commercialization milestones totaling up to €670 million plus royalties on future product sales.
 
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.