Drug intelligence / Profile preview

etrumadenant + sacituzumab govitecan + zimberelimab

Development stage
Phase 2
Lead developer
Arcus Biosciences
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This is an investigational combination therapy comprising three agents with distinct mechanisms of action, under evaluation for the treatment of advanced solid tumors, particularly metastatic colorectal cancer.

  • Etrumadenant is a small molecule dual antagonist of adenosine A2a and A2b receptors, designed to block adenosine-mediated immunosuppression in the tumor microenvironment and restore antitumor immune cell activity.
  • Sacituzumab govitecan is an antibody-drug conjugate targeting Trop-2, delivering the cytotoxic payload SN-38 to Trop‑2–expressing cancer cells. It induces direct tumor cell death via DNA damage.
  • Zimberelimab is a monoclonal antibody that inhibits PD‑1, thereby enhancing T-cell–mediated antitumor immunity.

The combination aims to synergistically enhance immune-mediated tumor killing by simultaneously blocking immunosuppressive pathways and directly targeting tumor cells.

Other names
etrumadenantsacituzumab govitecanzimberelimab
02

Targets

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