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Imaradenant is an orally bioavailable small molecule antagonist of the adenosine A2A receptor (A2AR; ADORA2A), developed as a potential immuno-oncology drug. By selectively binding to and inhibiting A2AR on T lymphocytes, imaradenant blocks tumor-derived adenosine from suppressing immune cell activity. This mechanism restores T-cell proliferation and activation within the tumor microenvironment, thereby enhancing anti-tumor immune responses. Imaradenant has been investigated primarily for solid tumors such as non-small cell lung cancer and prostate cancer in clinical trials up to phase II. The drug was originally developed by Heptares Therapeutics (now Nxera Pharma) and further co-developed with AstraZeneca[1][3][4][7].
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