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Domain Therapeutics launches Phase 1-enabling studies on proprietary EP4 receptor antagonist program in cancer immunotherapy

2020.12.08

  • French-Canadian biotech company has nominated DT-9081 as development candidate and launched CMC activities

  • DT-9081 will be combined with immune checkpoint inhibitors (ICI) in the clinic with a view to increasing patient responsiveness

Strasbourg, France, December 8, 2020 – Domain Therapeutics, a biopharmaceutical company specializing in the discovery and development of new drugs targeting G Protein-Coupled Receptors (GPCRs) in immuno-oncology, neurology and rare diseases, today announces the launch of Phase 1-enabling studies with DT-9081, its proprietary EP4 receptor antagonist candidate for the treatment of cancers.

The investigation of immunosuppressive mechanisms responsible for the limited potency of immune checkpoints inhibitors (ICI) in the clinic led to the identification and inception of the GPCR EP4 receptor (EP4R). Some tumors release Prostaglandin E2, the natural ligand of EP4R that is expressed by some immune cells, which leads to tumor immune escape. This protumoral microenvironment can contribute to altering the activity of some ICIs. Thus, combining an EP4R antagonist with ICI may restore their therapeutic effect and further extend the population of patients responding to ICI therapies.

Domain Therapeutics has developed a proprietary small molecule based program designed to address Prostaglandin E2-mediated immunosuppression to ICI. The company has selected a development candidate and launched the Chemistry, Manufacturing and Controls (CMC) activities. Currently the company is converting the preclinical biomarkers into clinical biomarkers – to bring value to the clinical development.

“This step constitutes a significant company milestone; DT-9081 is the second immuno-oncology program to reach Phase 1-enabling studies – after the Adenosine Receptor antagonist drug candidate developed in partnership with Merck KGaA,” said Pascal Neuville, CEO at Domain Therapeutics. “Developing our proprietary drug candidates towards the clinical phase will significantly increase the value of Domain’s portfolio.”

About G Protein-Coupled Receptors

GPCRs belong to the family of membrane receptors and constitute one of the main classes of therapeutic targets for many indications. The binding of a hormone or a specific ligand to a receptor’s binding site activates one or several pathways for intracellular signaling. This enables the cell to provide an adapted response to the change in its environment. The drugs that target GPCRs represent about 30% of all treatments on the market, but only address 28% of the GPCRs. Thus, GPCRs remain largely underexploited to date. Domain Therapeutics uses its proprietary platforms, such as bioSens-AllTM, to validate GPCRs and propose novel drug candidates in immuno-oncology, neurology and rare diseases.