Drug intelligence / Profile preview

MK-7162

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

Overview

MK-7162 is an orally available small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), developed by Merck Sharp & Dohme for the treatment of solid tumors. By specifically targeting and binding to IDO1, a cytosolic enzyme responsible for the oxidation of tryptophan into the immunosuppressive metabolite kynurenine, MK-7162 decreases kynurenine levels in tumor cells. This inhibition restores and promotes the proliferation and activation of various immune cells—including dendritic cells, natural killer (NK) cells, and T lymphocytes—potentially leading to increased interferon production and a reduction in tumor-associated regulatory T-cells. The overall effect is reactivation of anti-tumor immunity suppressed by IDO1 overexpression in many cancers[1][6][4]. MK-7162 has been investigated primarily in phase 1 clinical trials as monotherapy or in combination with pembrolizumab for advanced or metastatic solid tumors[3][4].

02

Targets

IDO1 (Indoleamine 2,3-dioxygenase 1)

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