Preferred Label : Inupadenant;
NCIt synonyms : A2A Receptor Antagonist EOS100850;
NCIt definition : An orally bioavailable immune checkpoint inhibitor and antagonist of the adenosine
A2A receptor (A2AR; ADORA2A), with potential immunomodulating and antineoplastic activities.
Upon administration, inupadenant selectively binds to and inhibits A2AR expressed
on T-lymphocytes. This prevents tumor-released adenosine from interacting with the
A2A receptors, thereby blocking the adenosine/A2AR-mediated inhibition of T-lymphocytes.
This results in the proliferation and activation of T-lymphocytes, and stimulates
a T-cell-mediated immune response against 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 overproduced by cancer
cells and plays a key role in immunosuppression.;
UNII : HQ700V0X06;
CAS number : 2246607-08-7;
Molecule name : EOS-100850; EOS 100850;
NCI Metathesaurus CUI : CL1413218;
Origin ID : C172109;
UMLS CUI : C5557477;
Semantic type(s)
- concept_is_in_subset
- has_target
