On April 7, 2024 iTeos Therapeutics, Inc. (Nasdaq: ITOS), a clinical-stage biopharmaceutical company pioneering the discovery and development of a new generation of immuno-oncology therapeutics for patients, reported a poster presentation of preclinical data on EOS-984, a potential first-in-class small molecule inhibitor targeting the equilibrative nucleoside transporter 1 (ENT1) in oncology, at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting, being held April 5-10, 2024 in San Diego, California (Press release, iTeos Therapeutics, APR 7, 2024, View Source [SID1234641843]).

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Based on the Company’s discovery and characterization of ENT1 in adenosine-mediated immunosuppression, this novel mechanism allows for the intracellular accumulation of adenosine, which then suppresses proliferation and effector function of T cells in the high adenosine tumor microenvironment. In mouse models, deletion of ENT1 led to potent control of tumor proliferation and increased CD8+ T cell frequency, proliferation, and cytokine production within tumors, further supporting ENT1’s role in tumor growth. In preclinical studies, blockade of intracellular adenosine accumulation by EOS-984 enabled proliferation of memory T cells and TILs despite high adenosine concentrations, resulting in the restoration of T cell function and enhanced tumor cell killing. Furthermore, combination of EOS-984 with anti-PD-1 therapy synergistically led to the control of tumor growth in a humanized mouse model of triple negative breast cancer resistant to anti-PD-1 blockade. Due to its mechanism of action, EOS-984 holds potential as a combination partner beyond anti-PD-1 therapy, including other immuno-oncology agents, cell therapies, and bispecific T cell engagers.

EOS-984 is currently in the dose escalation portion of a Phase 1 trial in advanced malignancies. Topline data from the Phase 1 trial is anticipated in the second half of 2024.

Abstracts are available on AACR (Free AACR Whitepaper)’s website located at www.aacr.org. Posters will be archived in the Investors section of the Company’s website located at www.iteostherapeutics.com.

Poster Presentation Details

Title: "Inhibition of equilibrative nucleoside transporter 1 relieves intracellular adenosine-mediated immune suppression"
Session Title: Experimental and Molecular Therapeutics: Tumor Microenvironment
Abstract Number: 734
Date and Time: Sunday, April 7, 2024, 1:30 p.m. – 5:00 p.m. PT
Location: Poster Section 29

About iTeos Therapeutics, Inc.

iTeos Therapeutics is a clinical-stage biopharmaceutical company pioneering the discovery and development of a new generation of immuno-oncology therapeutics for patients. iTeos Therapeutics leverages its deep understanding of tumor immunology and immunosuppressive pathways to design novel product candidates with the potential to restore the immune response against cancer. The Company’s innovative pipeline includes three clinical-stage programs targeting novel, validated immunosuppressive pathways designed with optimized pharmacologic properties for improved clinical outcomes, including the TIGIT/CD226 axis and the adenosine pathway. iTeos Therapeutics is headquartered in Watertown, MA with a research center in Gosselies, Belgium.

About EOS-984

EOS-984 is a potential first-in-class small molecule targeting the equilibrative nucleoside transporter 1 (ENT1) designed to inhibit the immunosuppressive activity of adenosine and restore immune cell proliferation. The therapeutic candidate has the potential to fully reverse the profound immunosuppressive action of adenosine on T and B cells and is in Phase 1 development.