Chemistry:Zavondemstat
From HandWiki
Zavondemstat (TACH101, QC8222) is a drug which acts as an inhibitor of the enzyme lysine-specific demethylase 4 (KDM4). It is described as a pan-KDM4 inhibitor, being active at all four isoforms KDM4A, KDM4B, KDM4C and KDM4D, which show functional redundancy so older inhibitors selective for just one isoform have failed to be effective. Zavondemstat is being researched for the treatment of certain forms of cancer and is in early stage clinical trials.[1][2][3][4]
References
- ↑ "TACH101, a first-in-class pan-inhibitor of KDM4 histone demethylase". Anti-Cancer Drugs 34 (10): 1122–1131. November 2023. doi:10.1097/CAD.0000000000001514. PMID 37067993.
- ↑ Chandhasin C, Perabo F, Dai Y, DiMascio L, Mehta RK, Hassan MK, Nyati MK. 245 (PB233): Histone methylation changes of H3K9 and H3K36 in PBMCs as pharmacodynamic biomarkers for Zavondemstat (TACH101), a paninhibitor of KDM4 histone lysine demethylase. European Journal of Cancer 2024; 211: 114763.
- ↑ "Phase 1 study of zavondemstat (TACH101), a first-in-class KDM4 inhibitor, in patients with advanced solid tumors". The Oncologist 30 (7). July 2025. doi:10.1093/oncolo/oyaf169. PMID 40580997.
- ↑ "A patent review of KDM4 histone demethylase inhibitors (2014-present)". Expert Opinion on Therapeutic Patents: 1–17. January 2026. doi:10.1080/13543776.2026.2614491. PMID 41504014.
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