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LSD1 inhibitors for anticancer therapy: an updated patent review (2022–2025)
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DOI：10.1080/13543776.2026.2636040.png)
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Abstract
En 中文
Lysine-specific demethylase 1 (LSD1) is a key epigenetic enzyme relying on flavin adenine dinucleotide to regulate gene expression via histone H3 demethylation and non-histone substrate modification. Discovered in 2004, it overturned the view that histone modifications are irreversible. Abnormal LSD1 overexpression drives solid tumor and hematological malignancy initiation, progression, and drug resistance, making it a key oncology target.
This review discusses recent innovations in LSD1 inhibitor development, focusing on small-molecule patents published from 2022 to 2025. A systematic search of SciFinder, Derwent Innovation, and WIPO databases was conducted for this period. It categorizes these novel inhibitors into six classes and summarizes their structural features, biological data, design strategies and LSD1 interaction mechanisms.
In recent years, LSD1 inhibitors have demonstrated structural diversification, innovative mechanisms, and expanded indications. Concurrently, breakthroughs have been achieved in optimizing structure, mechanism of action, dual-target strategies, selectivity and safety, and indications. Future efforts should focus on further validating dual-target strategies, and elucidating binding mechanisms to advance their application as a core targeted therapy in epigenetics for more malignant tumors therapy.
Keywords:
LSD1 (lysine-specific demethylase 1)
inhibitors design strategies
anticancer therapy
small-molecule inhibitors
epigenetic regulation
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