Preferred Label : Etrumadenant;
NCIt synonyms : A2AR/A2BR Antagonist AB928; Dual A2AR/A2BR Antagonist AB928; Adenosine A2A/A2B Receptor Antagonist AB928;
NCIt definition : An orally bioavailable antagonist of both the immunomodulatory checkpoint molecules
adenosine A2A receptor (A2AR; ADORA2A) and A2B receptor (A2BR; ADORA2B), with potential
immunomodulating and antineoplastic activities. Upon administration, etrumadenant
competes with tumor-released adenosine for binding to A2AR and A2BR expressed on numerous
intra-tumoral immune cells, such as dendritic cells (DCs), natural killer (NK) cells,
macrophages and T-lymphocytes. The binding of AB928 to A2AR and A2BR inhibits A2AR/A2BR
activity and prevents adenosine-A2AR/A2BR-mediated signaling. A2AR/A2BR inhibition
activates and enhances the proliferation of various immune cells, abrogates the adenosine-mediated
immunosuppression in the tumor microenvironment (TME) and activates the immune system
to exert anti-tumor immune responses against cancer cells, which leads to tumor cell
killing. A2AR and A2BR, G protein-coupled signaling receptors, are expressed on the
cell surfaces of numerous immune cells. Adenosine is often overproduced by tumor cells
and plays a key role in immunosuppression and tumor cell proliferation.;
UNII : W0ZE0NT8IF;
InChIKey : BUXIAWLTBSXYSW-UHFFFAOYSA-N;
CAS number : 2239273-34-6;
Molecule name : AB 928; AB-928;
NCI Metathesaurus CUI : CL951401;
Origin ID : C159564;
UMLS CUI : C5446344;
Semantic type(s)
- concept_is_in_subset
- has_target
