TACH101: A First-in-Class KDM4-Targeted Therapy
A Critical Driver of Tumorigenesis and Novel Target for Cancer Therapy
TACH101 is a first-in-class, orally available, selective, and potent small-molecule inhibitor of the entire KDM4 protein family. This epigenetic regulator, comprising KDM4A, B, C, and D histone demethylases, drives tumorigenic pathways such as gene overexpression, genomic instability, uncontrolled cell proliferation, inhibition of apoptosis, and metastasis.
Discovered using our proprietary single-cell genomic analysis technology, TACH101 has demonstrated significant preclinical activity by effectively blocking the proliferation of multiple cancer cell lines and patient-derived organoid models, which are 3D tissue cultures derived from cancer stem cells that KDM4 also helps maintain for self-renewal.
In animal xenograft models across various cancer types, including colorectal, esophageal, breast, and lymphoma, TACH101 treatment reduced tumor growth by up to 100% and, importantly, reduced the number of tumor-initiating cancer stem cells responsible for relapses, metastases, and chemotherapy resistance.
KDM4 overexpression is associated with these and other cancer types, like prostate, making it an important novel therapeutic target. TACH101 (formerly QC8222) is currently in a first-in-human Phase 1 clinical trial (NCT05076552) for the treatment of advanced or metastatic cancers, making it the only KDM4 inhibitor in development.