• Merck KGaA, Darmstadt, Germany’s decision to enter regulatory development with drug candidate triggers first development milestone

 • Candidate will be combined with Immune Checkpoint Inhibitors (ICI) for treatment of various cancers

Strasbourg, France, May 4, 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, announces today that the decision of Merck KGaA, Darmstadt, Germany, to enter into a regulatory phase of drug development with its candidate, triggers an undisclosed milestone payment to Domain Therapeutics.

The candidate was identified during a collaboration with Merck KGaA, Darmstadt, Germany, that was initiated in 2017, making Domain Therapeutics eligible for more than €240 million ($261M) in development milestones, as well as undisclosed royalties. The compound is an orally available small molecule antagonist of adenosine receptors. It fulfils all the criteria defined by Merck KGaA, Darmstadt, Germany, to become a valuable drug candidate and to be developed as a differentiated immunotherapeutic agent in multiple cancers.

The adenosine receptor antagonist program brought to the collaboration by Domain Therapeutics was the first asset from its immuno-oncology franchise, which has significantly expanded over the years. Today, the company has other assets from hitto-lead to candidate stage and has secured exclusive access to a target validation approach to identify GPCR modulation in the immuno-oncology field.

“This new adenosine receptor antagonist is one of the strategic assets in our immuno-oncology pipeline,” said Joern-Peter Halle, senior vice president, head of immuno-oncology research at Merck KGaA, Darmstadt, Germany. “It results from a successful and productive collaboration between the Domain and Merck KGaA, Darmstadt, Germany teams. We are eager to see the compound progressing through regulatory development and entering the clinic for the benefit of cancer patients.”

“We are delighted to have contributed to the strengthening of Merck KGaA, Darmstadt, Germany’s portfolio in immuno-oncology with a new adenosine receptor antagonist,” said Pascal Neuville, CEO of Domain Therapeutics. “This is a great achievement for Domain. It illustrates its capacity to discover and deliver valuable clinical candidates and highlights Domain’s innovation capacity in immunotherapies.”

About adenosine receptor antagonists in immuno-oncology

Adenosine is a powerful immunosuppressive substance produced inside tumors as a result of rapid cancer cell turnover. In some cases, it is responsible for resistance to certain anti-tumor interventions, such as chemotherapy and radiation. The adenosine receptors, expressed on the surface of immune cells, mediate the immunosuppressive effects of adenosine. The adenosine-driven impairment of tumor-infiltrating lymphocytes (mainly CD8+ T cells and NK cells) and myeloid cells (dendritic cells, macrophages), mediated by adenosine receptors, requires the development of specific inhibitors. For the last few years, the pharma industry has been investigating the benefit of combining adenosine receptor antagonists with ICI in order to decrease adenosinemediated resistance and restore ICI antitumor activity.

About Domain Therapeutics

Domain Therapeutics is a biopharmaceutical company dedicated to the discovery and development of new drug candidates targeting G Protein-Coupled Receptors (GPCRs), one of the most important classes of drug targets. With teams at work in Europe and North America, Domain creates a pipeline of high-value programs in immuno-oncology, neurology and rare diseases which are developed as proprietary programs up to early clinical phases or in collaboration with pharma partners. Some programs are also developed through asset-centric companies. These vehicles benefit from dedicated teams and targeted investments for a focused development. Exit is through a trade sale at an appropriate inflection point.

www.domaintherapeutics.com

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