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MK-1088 (Merck & Co.)
- Development stage
- Discontinued
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MK-1088 is an orally bioavailable, small-molecule dual antagonist of the adenosine A2A and A2B receptors. Developed by Merck & Co., the compound was designed to target the immunosuppressive effects of elevated adenosine levels in the tumor microenvironment (TME). Adenosine agonism of A2A and A2B receptors on T cells and myeloid cells suppresses anti-tumor immune responses. By blocking both receptors, MK-1088 aims to restore T-cell function and enhance anti-tumor immunity, particularly when combined with immune checkpoint inhibitors like pembrolizumab. MK-1088 was evaluated in Phase 1/2 clinical trials for advanced solid tumors, but development was discontinued for business reasons.
- Other names
- A2A/2B dual receptor antagonistA2A/A2B dual receptor antagonistdual A2A/A2B receptor antagonist
02
Targets
ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)
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