MENU

 
 

 

IMMUNO-ONCOLOGY

A2A/A2B

  • Extracellular adenosine in the TME may limit antitumor activity of T cells and myeloid cells through A2AR-mediated cAMP signaling in the cells.1,2
  • A2BR, having lower affinity to adenosine compared to A2AR, is also involved in immune suppression, tumor proliferation, tumor angiogenesis, tumor cell invasion, and metastasis in adenosine-high TME, whereas A2BR acts complementary or compensatory to A2AR.3,4
  • Dual A2AR/A2BR antagonism is expected to limit adenosine-driven immuno-suppression/tumor promotion at the receptor level regardless of the mechanism of adenosine accumulation.
  • M1069 is an investigational small molecule, dual adenosine receptor antagonist. M1069 is thought to block immunosuppressive signaling through the A2AR/A2BR adenosine receptors, thus enhancing antitumor immune activity.

TARGETS UNDER INVESTIGATION

PD-L1

LEARN MORE

TIGIT

LEARN MORE

VIEWPOINTS ON CANCER

Viewpoints In Cancer

Explore what's next in oncology with insights and perspectives.

EMD Serono is the healthcare business of Merck KGaA, Darmstadt, Germany in the U.S. and Canada.

STAY CURIOUS

Investigational compounds are not approved by any health authority. Safety and efficacy have not been established.

Abbreviations:

A2A/A2B, A2A and A2B receptors; AMP, adenosine monophosphate; ATP, adenosine triphosphate; cAMP, cyclic adenosine monophosphate; PD-L1, programmed death-ligand 1; TIGIT, T-cell immunoglobulin; TME, tumor microenvironment.

References:

  1. Leone RD, Emens LA. Targeting adenosine for cancer immunotherapy. J Immunother Cancer. 2018;6(1):57. 
  2. Augustin RC, Leone RD, Naing A, et al. Next steps for clinical translation of adenosine pathway inhibition in cancer immunotherapy. J Immunother Cancer. 2022;10(2):e004089.
  3. Novitskiy SV, Ryzhov S, Zaynagetdinov R, et al. Adenosine receptors in regulation of dendritic cell differentiation and function. Blood. 2008;112(5):1822-1831. 
  4. Ryzhov S, Novitskiy SV, Zaynagetdinov R, et al. Host A(2B) adenosine receptors promote carcinoma growth. Neoplasia. 2008;10(9):987-995. 

© 2023 Merck KGaA, Darmstadt, Germany and/or its affiliates. All rights reserved. EMD Serono, Inc. is the healthcare business of Merck KGaA, Darmstadt, Germany in the US and Canada.

US-MULO-00051
Last updated 07/2023

Are You a Healthcare Professional?

Yes
No