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EOS-984 is a potential first-in-class small molecule inhibitor of equilibrative nucleoside transporter 1 (ENT1, also known as SLC29A1), developed by iTeos Therapeutics for oncology indications. By selectively inhibiting ENT1, EOS-984 blocks the cellular uptake of adenosine, a metabolite that accumulates in the tumor microenvironment and suppresses immune cell function. This inhibition restores T cell proliferation and activity even under high adenosine conditions, thereby enhancing anti-tumor immune responses. Preclinical studies have shown that deletion or blockade of ENT1 leads to increased CD8+ T cell frequency, proliferation, cytokine production within tumors, and improved tumor control. In combination with anti-PD-1 therapy (such as pembrolizumab), EOS-984 has demonstrated synergistic effects in preclinical models resistant to checkpoint inhibitors. The drug is currently being evaluated in Phase 1 clinical trials for advanced solid tumors and is administered orally[2][3][4][5][6][7][8][9].
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