Taminadenant

**Semantic type:** Amino Acid, Peptide, or Protein|Pharmacologic Substance

**Definition:** An orally bioavailable adenosine A2A receptor (A2AR) antagonist, with potential antineoplastic activity. Upon administration, A2AR antagonist PBF-509 selectively binds to and inhibits A2AR expressed on T-lymphocytes. This abrogates the adenosine/A2AR-mediated inhibition of T-lymphocytes and activates a T-cell-mediated immune response against tumor cells, thereby reducing proliferation of susceptible tumor cells. A2AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of T-cells and, upon activation by adenosine, inhibits their proliferation and activation. Adenosine is often produced in excess by cancer cells.

**Synonyms:** - 4-Pyrimidinamine, 5-Bromo-2,6-di-1H-pyrazol-1-yl- - A2AR Antagonist PBF-509 - PBF-509 - TAMINADENANT