In 2017, Domain Therapeutics and Merck KGaA (Darmstadt, Germany) entered into collaboration and licensing agreement for the development of adenosine receptor antagonist drugs specifically designed for oncology and immuno-oncology (see press release).

Program description

Adenosine A2AR antagonist

  • Discovery
  • Candidate
  • Preclinical
  • Clinical

Adenosine release in the tumor-microenvironment has been recently identified as a key cancer immune evasion mechanism. In 2014, a publication (Mittal D et al; Cancer Res. 2014) suggested that combining an A2AR-antagonist with an anti-PD1 monoclonal antibody is able to significantly reduce metastatic burden (also demonstrated with anti-CTLA 4 and anti-TIM 3) and to extend survival in animal cancer models.

We identified a novel chemical series of A2AR-antagonists presenting clear differentiating points over the standard A2AR-antagonists initially developed for CNS indications. In early 2017, Domain Therapeutics entered into a license and collaboration agreement with Merck to develop A2AR antagonists in immuno-oncology.

Other Programs

EP4R antagonist for immuno-oncology


PAR2 negative allosteric modulator for rare inflammatory diseases