LSD1 inhibitors
Drugs against the histone demethylase LSD1, which keeps blood and neuroendocrine cancer cells from maturing; being tested in myelofibrosis, leukaemia and small cell lung cancer.
Overview
Lysine-specific demethylase 1 (LSD1, gene KDM1A) removes methyl marks from histone H3 and supports the undifferentiated state of acute myeloid leukaemia blasts and small cell lung cancer cells. Inhibitors such as bomedemstat, iadademstat and pulrodemstat have shown differentiation responses and platelet-lowering effects, leading to trials in essential thrombocythaemia and myelofibrosis as well as combination studies in AML and small cell lung cancer. Thrombocytopenia is the on-target dose-limiting effect.
How it works
Irreversible or reversible inhibitors block LSD1's demethylase activity and its scaffolding role with GFI1, releasing differentiation programmes.
- Differentiation rather than cytotoxicity
- Activity in myeloproliferative neoplasms
- Thrombocytopenia
- No approval yet
- Single-agent solid tumour activity limited
Latest papers
topQuery for this technology: (TITLE:"LSD1 inhibitors" OR ABSTRACT:"LSD1 inhibitors") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about LSD1 inhibitors, not a curated reading list.
Similar pages
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