Drug intelligence / Profile preview

A2AR inhibitor

Development stage
Unknown
Lead developer
Novartis
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Oral, Intravenous
01

Overview

Adenosine A2A receptor (A2AR) inhibitors are a class of therapeutic agents designed to block the immunosuppressive effects of adenosine, a nucleoside that accumulates at high levels in the hypoxic tumor microenvironment. Adenosine binds to A2AR on the surface of various immune cells, including T cells, natural killer (NK) cells, and dendritic cells, leading to increased intracellular cAMP levels that inhibit immune activation and effector functions. By antagonizing this metabolic checkpoint, A2AR inhibitors aim to restore anti-tumor immunity and are frequently evaluated in combination with other immunotherapies, such as PD-1/PD-L1 inhibitors or CAR-T cell therapies, to enhance efficacy and overcome resistance. Beyond oncology, A2AR inhibition is also explored for its potential in treating neurodegenerative disorders like Parkinson's disease and modulating inflammatory responses in infectious and ischemic conditions.

Other names
Adenosine A2A receptor inhibitorA2A receptor antagonistA-2A receptor antagonistA 2A receptor antagonistADORA2A inhibitorADORA-2A inhibitorADORA 2A inhibitorA2AR antagonistA-2AR antagonistA 2AR antagonist
02

Targets

ADORA3 (Adenosine A3 receptor)ADORA2A (Adenosine A₂A Receptor)ADORA1 (Adenosine receptor A1 subtype)ADORA2B (Adenosine A2B receptor)

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