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our Premium Content: News alerts, weekly reports and conference plannersDRUG:
MK-1088
i
Other names: MK-1088
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Company:
Merck (MSD)
Drug class:
Adenosine A2A receptor antagonist, Adenosine A2B receptor antagonist
Related drugs:
8d
Discovery of MK-1088 as a Potent A2A/A2B Adenosine Receptor Dual-Antagonist for Cancer Immunotherapy. (PubMed, J Med Chem)
Simultaneous blockade of the downstream effects mediated by both receptor subtypes with a dual inhibitor has the potential to reverse adenosine-mediated suppression of tumor immune surveillance as either a single-agent treatment or in combination with other immunotherapy agents such as anti-PD-1/PD-L1 monoclonal antibodies. This publication describes the discovery and optimization of a novel series of potent and selective dual A2AR/A2BR antagonists, resulting in compound 46 (MK-1088) being identified for progression to human clinical studies.
Journal
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ADORA2A (Adenosine A2a Receptor)
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MK-1088
3years
A Study of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors (MK-1088-002) (clinicaltrials.gov)
P1/2, N=80, Active, not recruiting, Merck Sharp & Dohme LLC | Recruiting --> Active, not recruiting | Trial completion date: Nov 2025 --> May 2025 | Trial primary completion date: Nov 2025 --> May 2025
Enrollment closed • Trial completion date • Trial primary completion date • Combination therapy • Metastases
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Keytruda (pembrolizumab) • MK-1088
almost4years
A Phase 1/Phase 2 Study to Evaluate the Safety and Tolerability of MK-1088 as Monotherapy/ single agent and in Combination with Pembrolizumab in Participants with Advanced Solid Tumors (clinicaltrialsregister.eu)
P1/2, N=80, Ongoing, Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc
New P1/2 trial • Combination therapy
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CD4 (CD4 Molecule)
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Keytruda (pembrolizumab) • MK-1088
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