Etrumadenant  (Synonyms: AB928)

Etrumadenant (AB928) is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. Etrumadenant relieves adenosine-mediated immune suppression. Etrumadenant has immunomodulatory and antitumor activities^[1][2].

A2aR/A2bR^[1]

In human in vitro cell cultures, moDC differentiated in the presence of adenosine showed a decreased ability to stimulate IFN-γ secretion from allogenic CD4+ T-cells in a MLR. This suppression is significantly reversed by addition of Etrumadenant. Multiplexed gene expression profiling using NanoString identified a cassette of 39 genes that are regulated by adenosine during moDC differentiation. Etrumadenant shows rescue of these gene expression changes^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Concurrent treatment with Etrumadenant and chemotherapy results in significantly reduced tumor volume in vivo using AT3-OVA tumors; Similar results are observed for the combination of Etrumadenant and NSC 266046. AB928 is also capable of suppressing growth of B16-F10 tumors both as a single agent or in combination with α-PD-1 therapy. Etrumadenant increases the antitumor immune response leading to suppressed tumor growth and increased immune cell infiltration in mouse syngeneic tumors^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

426.47

Solid

C₂₃H₂₂N₈O

2239273-34-6

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Room temperature in continental US; may vary elsewhere.

• [1]. Seitz L, et al. Safety, tolerability, and pharmacology of AB928, a novel dual adenosine receptor antagonist, in a randomized, phase 1 study in healthy volunteers. Invest New Drugs. 2019 Aug;37(4):711-721.  [Content Brief]

  [2]. Daniel DiRenzo, et al. AB928, a dual antagonist of the A2aR and A2bR adenosine receptors, relieves adenosine-mediated immune suppression [abstract].