Drug intelligence / Profile preview

MK-1088

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-1088 is an investigational small molecule drug developed as a dual inhibitor of the adenosine A2A and A2B receptors. It is designed as an immunotherapy for the treatment of advanced solid tumors, including those that are metastatic or unresectable. By blocking both A2A and A2B receptors, MK-1088 aims to counteract T-cell inhibition caused by high levels of adenosine in the tumor microenvironment, thereby enhancing anti-tumor immune responses. Preclinical studies have shown antitumor activity when combined with PD-1 inhibitors such as pembrolizumab. MK-1088 is administered orally and has demonstrated dose-proportional pharmacokinetics with a half-life of approximately 11 hours in clinical studies[1][6]. It is currently being evaluated in phase 1/phase 2 trials both as monotherapy and in combination with pembrolizumab for patients whose tumors have not responded to conventional therapies[3][4][5].

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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