Drug intelligence / Profile preview

GTN057

Development stage
Preclinical
Lead developer
Keio University
Modality
Small Molecules
01

Overview

GTN057 is a small molecule derivative of Komaroviquinone (KQN) that acts as an inducer of immunogenic cell death (ICD). Developed by researchers at Keio University and the National Cancer Center Research Institute in Japan, it is primarily being investigated for the treatment of multiple myeloma. GTN057 triggers the hallmarks of ICD, including the cell surface expression of calreticulin (CRT) and the release of ATP and HMGB1 from cancer cells. Its mechanism of action involves the facilitation of reactive oxygen species (ROS) production and the up-regulation of endoplasmic reticulum (ER) stress-related genes. By inducing ICD, GTN057 promotes the maturation of dendritic cells (DCs)—evidenced by increased expression of HLA-DR, CD80, and CD83—and the subsequent activation of T cells, potentially offering synergistic therapeutic effects when used in combination with other immunotherapies.

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