Selective Antagonists of the A2B Adenosine Receptor

Using X-ray structure-based molecular design, leadXpro has discovered, optimised and patented two new series of selective antagonists of the A2B adenosine receptor.

The A2B adenosine receptor is an important target for cancer immunotherapy, with no drugs currently on the market. Using X-ray structure-based molecular design, leadXpro has discovered and patented new antagonists of A2B.

Biophysical and cellular functional assays demonstrate the high potency of the compounds as well as the excellent selectivity versus other adenosine receptors, which was achieved with the team’s cutting-edge methods of rational design. Lead optimization efforts have improved ADME properties, such as the metabolic stability, and efficacy in disease models has also been established.

Partnering discussions are ongoing to co-develop leadXpro A2B antagonist program. Please contact us at for more information.

A2B gpcr_s
Structural model of A2B, an important target in immuno-oncology


Poster presented at the RSC/SCI Symposium on GPCRs in Verona, Italy (5-7 October, 2022):
Discovery of selective inhibitors of A2B adenosine receptors