Imaradenant (AZD-4635; HTL1071)

Description: AZD-4635 (also known as HTL-1071) is a novel, potent, selective, orally bioavailable small molecule inhibitor of the adenosine A2A receptor (A2AR) (Ki = 1.7 nM) with potential anticancer activity. It can be used as a potential cancer immonotherapy agent by binding to human A2AR and shows > 30-fold selectivity over other adenosine receptors. The blockade of A2aR signaling by AZD4635 can reduce tumor burden and enhance antitumor immunity. AZD4635 is currently being studied in a Phase 1 clinical trial as a single agent and in combination with durvalumab (anti-PD-L1 Ab) in patients with solid malignancies. Accumulation of extracellular adenosine within the microenvironment is a strategy exploited by tumors to escape immunosurveillance.

References: AACR; Cancer Res 2017; 77(13 Suppl):Abstract nr 5580.