Ciforadenant (CPI-444; V81444)

Description: Ciforadenant (also known as CPI-444 and V81444) is a potent, selective and orally bioactive small molecule inhibitor of the adenosine-A2a receptor (A2AR) on T-lymphocytes. Ciforadenant is currently in a Phase I clinical trial as a single agent and in combination with atezolizumab, a PD-L1 inhibitor against various solid tumors. Ciforadenant is able to induce antitumor responses. Upon oral administration, Ciforadenant binds to adenosine A2A receptors expressed on the surface of immune cells, including T-lymphocytes, natural killer (NK) cells, macrophages and dendritic cells (DCs), which prevents tumor-released adenosine from interacting with the A2A receptors on these key immune surveillance cells, thereby abrogating adenosine-induced immunosuppression in the tumor microenvironment.

References: Cancer Immunoly Research. September 25-28, 2016.