TT-702

TT-702 is an orally bioavailable small molecule prodrug and selective antagonist of the adenosine A2B receptor (A2BR, also known as ADORA2B), an immunomodulatory checkpoint molecule. After administration, TT-702 is converted into its active form, TT-478, which blocks the A2B receptor. This inhibition prevents activation by elevated adenosine levels in the tumor microenvironment—a process that otherwise promotes tumor growth and suppresses immune cell activity. By blocking this pathway, TT-702 aims to enhance anti-tumor immune responses and inhibit cancer cell proliferation. The drug is being developed primarily for advanced or metastatic solid tumors where standard treatments have failed. It is currently under investigation both as a monotherapy and in combination with other agents such as androgen receptor antagonists (e.g., darolutamide) or immunotherapies[1][3][4][5][8].