Drug intelligence / Profile preview

etrumadenant + zimberelimab + quemliclustat

Development stage
Unknown
Lead developer
Arcus Biosciences
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

**etrumadenant + zimberelimab + quemliclustat** is an investigational combination therapy for cancer. - **Etrumadenant** is an orally bioavailable, selective, dual antagonist of the adenosine A2a and A2b receptors designed to block adenosine-mediated immunosuppression, thereby enhancing antitumor immunity. - **Zimberelimab** is a monoclonal antibody targeting PD-1, acting as an immune checkpoint inhibitor. - **Quemliclustat** is an investigational small-molecule inhibitor of CD73, an enzyme controlling extracellular adenosine formation; its inhibition reduces adenosine-mediated immune suppression within the tumor microenvironment and may boost the effectiveness of immunotherapy. Developed by Arcus Biosciences (with Gilead Sciences as a partner for a subset of programs), this combination is under active clinical investigation, primarily for metastatic colorectal cancer and pancreatic cancer. Key studies include the ARC-9 (in metastatic colorectal cancer) and ARC-8/PRISM-1 (in pancreatic cancer, primarily for quemliclustat). The regimen is not yet approved for any indication[1][2][3][4][6][7].

02

Targets

ADORA2A (Adenosine A₂A Receptor)NT5E (Cluster of Differentiation 73)ADORA2B (Adenosine A2B receptor)PDCD1 (Programmed cell death protein 1 receptor)

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