Drug intelligence / Profile preview

EXS21546 + nivolumab

Development stage
Discontinued
Lead developer
Exscientia
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

EXS21546 + nivolumab is a **combination therapy** under clinical investigation for cancer. EXS21546 is an orally administered, highly potent and selective antagonist of the adenosine A2A receptor, designed to counteract adenosine-mediated immunosuppression in the tumor microenvironment. Nivolumab is a monoclonal antibody inhibitor of programmed death-1 (PD-1), an immune checkpoint. This combination aims to synergistically enhance anti-tumor immunity: EXS21546 blocks A2A receptor signaling to prevent suppression of immune cells in tumors, while nivolumab restores T-cell function by inhibiting PD-1. The combination was studied in a phase 1b/2a clinical trial for patients with advanced solid tumors, including non-small cell lung cancer (NSCLC) and renal cell carcinoma (RCC), but the study was terminated[1][3].[1][3][4][5]

02

Targets

ADORA2A (Adenosine A₂A Receptor)PDCD1 (Programmed cell death protein 1 receptor)

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