An adenosine A2A and A2B receptor dual antagonist
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AB-928 is an adenosine A2A and A2B receptor dual antagonist.1 It inhibits the ability of adenosine to suppress activation of human CD4 or CD8 T cells, as well as monocyte-derived dendritic cells, in vitro.2,3 AB-928, alone or in combination with doxorubicin , reduces tumor growth in an AT3-OVA syngeneic mouse model. It also acts synergistically with an anti-PD-1 antibody to reduce tumor growth in a B16/F10 syngeneic mouse model.
1.Seitz, L., Jin, L., Leleti, M., et al.Safety, tolerability, and pharmacology of AB928, a novel dual adenosine receptor antagonist, in a randomized, phase 1 study in healthy volunteersInvest. New Drugs37(4)711-721(2019) 2.Walters, M.J., Piovesan, D., Tan, J., et al.Abstract 5556: Combining adenosine receptor inhibition with AB928 and chemotherapy results in greater immune activation and tumor controlCancer Res.78(13 Suppl.)(2018) 3.DiRenzo, D., Piovesan, D., Tan, J., et al.Abstract A162: AB928, a dual antagonist of the A2aR and A2bR adenosine receptors, relieves adenosine-mediated immune suppressionCancer Immunol. Res.7(2 Suppl.)(2019)
5'-(N-Cyclopropyl)carboxamidoadenosine
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