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.
Zhang et al. (2026) studied this question.