A variety of cancers over-produce ligands of GPCRs expressed by specific immune cells to shut down their surveillance. It is the case for adenosine via A2a and A2b receptors, but also for prostaglandin E2 (PGE2), produced by COX2 positive tumors, that activates the prostaglandin receptor 4 (EP4R). Antagonizing EP4R is therefore a novel therapeutic approach to restore cancer recognition by the immune system and combat its progression.
EP4R antagonist (DT-9081)
Domain has designed a small molecule drug candidate DT-9081 which is progressing towards the clinic. Together with tumor profiling, the company has translated a complete and robust biomarker strategy monitoring target engagement and efficacy to support clinical development and cancer type prioritization.
This poster presents the complete characterization of Domain drug candidate benchmarked to EP4 antagonist molecules currently in the clinic and demonstrating a best-in-class potential.